|
Inhibitory concentration against the growth of 2SC/20 cell line after 72 hr of drug exposure by MTT test
|
Cricetulus griseus
|
517.0
nM
|
|
Journal : J. Med. Chem.
Title : Effects of isoprenoid analogues of SDB-ethylenediamine on multidrug resistant tumor cells alone and in combination with chemotherapeutic drugs.
Year : 2002
Volume : 45
Issue : 24
First Page : 5330
Last Page : 5339
Authors : Sidorova TA, Nigmatov AG, Kakpakova ES, Stavrovskaya AA, Gerassimova GK, Shtil AA, Serebryakov EP.
Abstract : Multidrug resistance (MDR) mediated by P-glycoprotein (Pgp) remains the major obstacle for successful treatment of cancer. Inhibition of Pgp transport is important for higher efficacy of anticancer drugs. Lipophilic cationogenic amines with at least one tertiary N atom, such as verapamil, are classical PgP-blocking agents. In a search for novel accessible compounds potent against MDR tumor cells, we synthesized a series of arylalkylamines that contain isoprenoid side chains of different length. Two out of seven new analogues of the known N,N'-bis(3,4-dimethoxybenzyl)-N-solanesylethylenediamine (SDB-ethylenediamine), namely, compounds with C10 and C15 side chains, at low micromolar concentrations were preferentially toxic for several mammalian tumor cell lines that acquired MDR during prolonged drug selection. Moreover, at noncytotoxic concentrations, these compounds potently sensitized MDR cells to Pgp substrates vinblastine and adriamycin. We conclude that these analogues of SDB-ethylenediamine may have dual therapeutic advantage because (i) they are preferentially toxic for MDR cells when administered alone and (ii) they potentiate the cytotoxicity of Pgp-transported anticancer drugs.
|
Inhibitory concentration against the growth of HET-SR-2SC-LNM cell line after 72 hr of drug exposure by MTT test
|
Cricetulus griseus
|
519.0
nM
|
|
Journal : J. Med. Chem.
Title : Effects of isoprenoid analogues of SDB-ethylenediamine on multidrug resistant tumor cells alone and in combination with chemotherapeutic drugs.
Year : 2002
Volume : 45
Issue : 24
First Page : 5330
Last Page : 5339
Authors : Sidorova TA, Nigmatov AG, Kakpakova ES, Stavrovskaya AA, Gerassimova GK, Shtil AA, Serebryakov EP.
Abstract : Multidrug resistance (MDR) mediated by P-glycoprotein (Pgp) remains the major obstacle for successful treatment of cancer. Inhibition of Pgp transport is important for higher efficacy of anticancer drugs. Lipophilic cationogenic amines with at least one tertiary N atom, such as verapamil, are classical PgP-blocking agents. In a search for novel accessible compounds potent against MDR tumor cells, we synthesized a series of arylalkylamines that contain isoprenoid side chains of different length. Two out of seven new analogues of the known N,N'-bis(3,4-dimethoxybenzyl)-N-solanesylethylenediamine (SDB-ethylenediamine), namely, compounds with C10 and C15 side chains, at low micromolar concentrations were preferentially toxic for several mammalian tumor cell lines that acquired MDR during prolonged drug selection. Moreover, at noncytotoxic concentrations, these compounds potently sensitized MDR cells to Pgp substrates vinblastine and adriamycin. We conclude that these analogues of SDB-ethylenediamine may have dual therapeutic advantage because (i) they are preferentially toxic for MDR cells when administered alone and (ii) they potentiate the cytotoxicity of Pgp-transported anticancer drugs.
|
Inhibition of electric eel AChE at 2 mg/ml by Ellman's method
|
Electrophorus electricus
|
10.15
%
|
|
Journal : Bioorg. Med. Chem.
Title : Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
Year : 2012
Volume : 20
Issue : 22
First Page : 6669
Last Page : 6679
Authors : Brunhofer G, Fallarero A, Karlsson D, Batista-Gonzalez A, Shinde P, Gopi Mohan C, Vuorela P.
Abstract : The presented project started by screening a library consisting of natural and natural based compounds for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. Active compounds were chemically clustered into groups and further tested on the human cholinesterases isoforms. The aim of the presented study was to identify compounds that could be used as leads to target two key mechanisms associated with the AD's pathogenesis simultaneously: cholinergic depletion and beta amyloid (Aβ) aggregation. Berberin, palmatine and chelerythrine, chemically clustered in the so-called isoquinoline group, showed promising cholinesterase inhibitory activity and were therefore further investigated. Moreover, the compounds demonstrated moderate to good inhibition of Aβ aggregation as well as the ability to disaggregate already preformed Aβ aggregates in an experimental set-up using HFIP as promotor of Aβ aggregates. Analysis of the kinetic mechanism of the AChE inhibition revealed chelerythrine as a mixed inhibitor. Using molecular docking studies, it was further proven that chelerythrine binds on both the catalytic site and the peripheral anionic site (PAS) of the AChE. In view of this, we went on to investigate its effect on inhibiting Aβ aggregation stimulated by AChE. Chelerythrine showed inhibition of fibril formation in the same range as propidium iodide. This approach enabled for the first time to identify a cholinesterase inhibitor of natural origin-chelerythrine-acting on AChE and BChE with a dual ability to inhibit Aβ aggregation as well as to disaggregate preformed Aβ aggregates. This compound could be an excellent starting point paving the way to develop more successful anti-AD drugs.
|
Inhibition of horse BChE at 2 mg/ml by Ellman's method
|
Equus caballus
|
10.78
%
|
|
Journal : Bioorg. Med. Chem.
Title : Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
Year : 2012
Volume : 20
Issue : 22
First Page : 6669
Last Page : 6679
Authors : Brunhofer G, Fallarero A, Karlsson D, Batista-Gonzalez A, Shinde P, Gopi Mohan C, Vuorela P.
Abstract : The presented project started by screening a library consisting of natural and natural based compounds for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. Active compounds were chemically clustered into groups and further tested on the human cholinesterases isoforms. The aim of the presented study was to identify compounds that could be used as leads to target two key mechanisms associated with the AD's pathogenesis simultaneously: cholinergic depletion and beta amyloid (Aβ) aggregation. Berberin, palmatine and chelerythrine, chemically clustered in the so-called isoquinoline group, showed promising cholinesterase inhibitory activity and were therefore further investigated. Moreover, the compounds demonstrated moderate to good inhibition of Aβ aggregation as well as the ability to disaggregate already preformed Aβ aggregates in an experimental set-up using HFIP as promotor of Aβ aggregates. Analysis of the kinetic mechanism of the AChE inhibition revealed chelerythrine as a mixed inhibitor. Using molecular docking studies, it was further proven that chelerythrine binds on both the catalytic site and the peripheral anionic site (PAS) of the AChE. In view of this, we went on to investigate its effect on inhibiting Aβ aggregation stimulated by AChE. Chelerythrine showed inhibition of fibril formation in the same range as propidium iodide. This approach enabled for the first time to identify a cholinesterase inhibitor of natural origin-chelerythrine-acting on AChE and BChE with a dual ability to inhibit Aβ aggregation as well as to disaggregate preformed Aβ aggregates. This compound could be an excellent starting point paving the way to develop more successful anti-AD drugs.
|
SANGER: Inhibition of human NCI-H1650 cell growth in a cell viability assay.
|
Homo sapiens
|
499.38
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H1651 cell growth in a cell viability assay.
|
Homo sapiens
|
505.3
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H1703 cell growth in a cell viability assay.
|
Homo sapiens
|
16.12
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H1734 cell growth in a cell viability assay.
|
Homo sapiens
|
17.42
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H2122 cell growth in a cell viability assay.
|
Homo sapiens
|
509.53
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H2170 cell growth in a cell viability assay.
|
Homo sapiens
|
162.42
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H2228 cell growth in a cell viability assay.
|
Homo sapiens
|
954.65
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H2342 cell growth in a cell viability assay.
|
Homo sapiens
|
13.83
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H292 cell growth in a cell viability assay.
|
Homo sapiens
|
803.16
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H358 cell growth in a cell viability assay.
|
Homo sapiens
|
372.71
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H522 cell growth in a cell viability assay.
|
Homo sapiens
|
425.69
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H64 cell growth in a cell viability assay.
|
Homo sapiens
|
641.01
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H650 cell growth in a cell viability assay.
|
Homo sapiens
|
0.5873
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-SNU-5 cell growth in a cell viability assay.
|
Homo sapiens
|
643.36
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NEC8 cell growth in a cell viability assay.
|
Homo sapiens
|
26.85
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NKM-1 cell growth in a cell viability assay.
|
Homo sapiens
|
7.647
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NMC-G1 cell growth in a cell viability assay.
|
Homo sapiens
|
11.85
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.
|
Homo sapiens
|
0.1391
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human OAW-42 cell growth in a cell viability assay.
|
Homo sapiens
|
831.82
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ONS-76 cell growth in a cell viability assay.
|
Homo sapiens
|
853.91
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human OVCAR-8 cell growth in a cell viability assay.
|
Homo sapiens
|
0.4763
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human PANC-03-27 cell growth in a cell viability assay.
|
Homo sapiens
|
316.39
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human PANC-10-05 cell growth in a cell viability assay.
|
Homo sapiens
|
256.06
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human PC-14 cell growth in a cell viability assay.
|
Homo sapiens
|
182.69
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human PF-382 cell growth in a cell viability assay.
|
Homo sapiens
|
426.16
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human PSN1 cell growth in a cell viability assay.
|
Homo sapiens
|
138.88
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human QIMR-WIL cell growth in a cell viability assay.
|
Homo sapiens
|
636.56
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human REH cell growth in a cell viability assay.
|
Homo sapiens
|
13.39
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RH-1 cell growth in a cell viability assay.
|
Homo sapiens
|
152.21
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RKO cell growth in a cell viability assay.
|
Homo sapiens
|
524.24
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RMG-I cell growth in a cell viability assay.
|
Homo sapiens
|
0.1319
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RPMI-2650 cell growth in a cell viability assay.
|
Homo sapiens
|
633.15
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RPMI-6666 cell growth in a cell viability assay.
|
Homo sapiens
|
445.05
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RS4-11 cell growth in a cell viability assay.
|
Homo sapiens
|
1.643
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human RT4 cell growth in a cell viability assay.
|
Homo sapiens
|
5.856
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SBC-5 cell growth in a cell viability assay.
|
Homo sapiens
|
623.55
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SCC-25 cell growth in a cell viability assay.
|
Homo sapiens
|
415.39
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SF295 cell growth in a cell viability assay.
|
Homo sapiens
|
21.39
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SF539 cell growth in a cell viability assay.
|
Homo sapiens
|
393.05
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SIG-M5 cell growth in a cell viability assay.
|
Homo sapiens
|
586.05
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SJRH30 cell growth in a cell viability assay.
|
Homo sapiens
|
414.11
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SK-CO-1 cell growth in a cell viability assay.
|
Homo sapiens
|
246.52
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SK-HEP-1 cell growth in a cell viability assay.
|
Homo sapiens
|
414.93
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SK-LU-1 cell growth in a cell viability assay.
|
Homo sapiens
|
998.68
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SK-MEL-30 cell growth in a cell viability assay.
|
Homo sapiens
|
376.88
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SK-UT-1 cell growth in a cell viability assay.
|
Homo sapiens
|
6.293
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SNG-M cell growth in a cell viability assay.
|
Homo sapiens
|
830.83
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SNU-387 cell growth in a cell viability assay.
|
Homo sapiens
|
924.72
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SNU-423 cell growth in a cell viability assay.
|
Homo sapiens
|
867.39
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SNU-449 cell growth in a cell viability assay.
|
Homo sapiens
|
388.51
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SR cell growth in a cell viability assay.
|
Homo sapiens
|
29.67
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SUP-T1 cell growth in a cell viability assay.
|
Homo sapiens
|
0.251
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW13 cell growth in a cell viability assay.
|
Homo sapiens
|
81.62
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW1573 cell growth in a cell viability assay.
|
Homo sapiens
|
137.15
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW1710 cell growth in a cell viability assay.
|
Homo sapiens
|
295.33
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW1783 cell growth in a cell viability assay.
|
Homo sapiens
|
249.25
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW48 cell growth in a cell viability assay.
|
Homo sapiens
|
546.12
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW954 cell growth in a cell viability assay.
|
Homo sapiens
|
9.572
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human SW982 cell growth in a cell viability assay.
|
Homo sapiens
|
417.43
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human Saos-2 cell growth in a cell viability assay.
|
Homo sapiens
|
171.96
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human T-24 cell growth in a cell viability assay.
|
Homo sapiens
|
719.91
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human 23132-87 cell growth in a cell viability assay.
|
Homo sapiens
|
131.46
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human 5637 cell growth in a cell viability assay.
|
Homo sapiens
|
28.97
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human 639-V cell growth in a cell viability assay.
|
Homo sapiens
|
219.56
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human 769-P cell growth in a cell viability assay.
|
Homo sapiens
|
122.8
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human 786-0 cell growth in a cell viability assay.
|
Homo sapiens
|
80.84
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human 8305C cell growth in a cell viability assay.
|
Homo sapiens
|
804.31
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A101D cell growth in a cell viability assay.
|
Homo sapiens
|
619.72
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A204 cell growth in a cell viability assay.
|
Homo sapiens
|
200.37
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A2058 cell growth in a cell viability assay.
|
Homo sapiens
|
807.68
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A2780 cell growth in a cell viability assay.
|
Homo sapiens
|
220.19
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A3-KAW cell growth in a cell viability assay.
|
Homo sapiens
|
716.92
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A375 cell growth in a cell viability assay.
|
Homo sapiens
|
71.1
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A388 cell growth in a cell viability assay.
|
Homo sapiens
|
877.18
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human A427 cell growth in a cell viability assay.
|
Homo sapiens
|
0.118
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ACHN cell growth in a cell viability assay.
|
Homo sapiens
|
374.63
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ACN cell growth in a cell viability assay.
|
Homo sapiens
|
808.34
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human AGS cell growth in a cell viability assay.
|
Homo sapiens
|
502.53
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ALL-PO cell growth in a cell viability assay.
|
Homo sapiens
|
986.27
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ARH-77 cell growth in a cell viability assay.
|
Homo sapiens
|
104.52
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BB30-HNC cell growth in a cell viability assay.
|
Homo sapiens
|
16.34
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BC-3 cell growth in a cell viability assay.
|
Homo sapiens
|
521.0
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BE-13 cell growth in a cell viability assay.
|
Homo sapiens
|
398.72
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BFTC-909 cell growth in a cell viability assay.
|
Homo sapiens
|
13.83
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BOKU cell growth in a cell viability assay.
|
Homo sapiens
|
136.98
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BPH-1 cell growth in a cell viability assay.
|
Homo sapiens
|
59.09
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human BV-173 cell growth in a cell viability assay.
|
Homo sapiens
|
854.87
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human C-33-A cell growth in a cell viability assay.
|
Homo sapiens
|
431.78
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human C-4-II cell growth in a cell viability assay.
|
Homo sapiens
|
381.31
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human C3A cell growth in a cell viability assay.
|
Homo sapiens
|
296.44
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CAKI-1 cell growth in a cell viability assay.
|
Homo sapiens
|
620.43
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CAL-12T cell growth in a cell viability assay.
|
Homo sapiens
|
258.51
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CAL-39 cell growth in a cell viability assay.
|
Homo sapiens
|
0.3147
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CAL-51 cell growth in a cell viability assay.
|
Homo sapiens
|
0.09899
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CAL-54 cell growth in a cell viability assay.
|
Homo sapiens
|
190.67
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CAL-85-1 cell growth in a cell viability assay.
|
Homo sapiens
|
0.1777
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human TE-10 cell growth in a cell viability assay.
|
Homo sapiens
|
783.12
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human TE-12 cell growth in a cell viability assay.
|
Homo sapiens
|
718.85
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human TE-8 cell growth in a cell viability assay.
|
Homo sapiens
|
376.69
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human TK10 cell growth in a cell viability assay.
|
Homo sapiens
|
998.68
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human U031 cell growth in a cell viability assay.
|
Homo sapiens
|
934.36
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human UM-UC-3 cell growth in a cell viability assay.
|
Homo sapiens
|
955.61
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human VA-ES-BJ cell growth in a cell viability assay.
|
Homo sapiens
|
260.47
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CCRF-CEM cell growth in a cell viability assay.
|
Homo sapiens
|
78.69
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CESS cell growth in a cell viability assay.
|
Homo sapiens
|
0.5457
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CHL-1 cell growth in a cell viability assay.
|
Homo sapiens
|
731.54
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CHP-212 cell growth in a cell viability assay.
|
Homo sapiens
|
147.74
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human COLO-668 cell growth in a cell viability assay.
|
Homo sapiens
|
0.02177
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human COR-L23 cell growth in a cell viability assay.
|
Homo sapiens
|
75.48
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human CTB-1 cell growth in a cell viability assay.
|
Homo sapiens
|
26.94
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human Ca-Ski cell growth in a cell viability assay.
|
Homo sapiens
|
798.23
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human Ca9-22 cell growth in a cell viability assay.
|
Homo sapiens
|
745.83
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human DEL cell growth in a cell viability assay.
|
Homo sapiens
|
479.88
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human DU-145 cell growth in a cell viability assay.
|
Homo sapiens
|
822.55
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human Daoy cell growth in a cell viability assay.
|
Homo sapiens
|
83.04
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human DoTc2-4510 cell growth in a cell viability assay.
|
Homo sapiens
|
378.34
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human EB2 cell growth in a cell viability assay.
|
Homo sapiens
|
691.03
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human EFM-19 cell growth in a cell viability assay.
|
Homo sapiens
|
14.77
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human EFO-27 cell growth in a cell viability assay.
|
Homo sapiens
|
571.04
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human EGI-1 cell growth in a cell viability assay.
|
Homo sapiens
|
772.32
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ES1 cell growth in a cell viability assay.
|
Homo sapiens
|
26.7
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ES4 cell growth in a cell viability assay.
|
Homo sapiens
|
38.26
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ES5 cell growth in a cell viability assay.
|
Homo sapiens
|
505.39
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ES6 cell growth in a cell viability assay.
|
Homo sapiens
|
406.25
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ES7 cell growth in a cell viability assay.
|
Homo sapiens
|
377.54
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ESS-1 cell growth in a cell viability assay.
|
Homo sapiens
|
187.44
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ETK-1 cell growth in a cell viability assay.
|
Homo sapiens
|
80.5
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human EW-13 cell growth in a cell viability assay.
|
Homo sapiens
|
292.08
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human EW-16 cell growth in a cell viability assay.
|
Homo sapiens
|
6.853
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human G-361 cell growth in a cell viability assay.
|
Homo sapiens
|
88.31
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human G-402 cell growth in a cell viability assay.
|
Homo sapiens
|
76.51
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human GAMG cell growth in a cell viability assay.
|
Homo sapiens
|
289.35
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human GB-1 cell growth in a cell viability assay.
|
Homo sapiens
|
390.11
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human GDM-1 cell growth in a cell viability assay.
|
Homo sapiens
|
228.45
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human GI-ME-N cell growth in a cell viability assay.
|
Homo sapiens
|
440.79
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human GOTO cell growth in a cell viability assay.
|
Homo sapiens
|
549.93
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human GT3TKB cell growth in a cell viability assay.
|
Homo sapiens
|
6.85
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human H4 cell growth in a cell viability assay.
|
Homo sapiens
|
320.74
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HAL-01 cell growth in a cell viability assay.
|
Homo sapiens
|
0.4527
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HC-1 cell growth in a cell viability assay.
|
Homo sapiens
|
992.91
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCC1395 cell growth in a cell viability assay.
|
Homo sapiens
|
500.94
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCC1569 cell growth in a cell viability assay.
|
Homo sapiens
|
604.49
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCC1806 cell growth in a cell viability assay.
|
Homo sapiens
|
8.543
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCC1937 cell growth in a cell viability assay.
|
Homo sapiens
|
0.254
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCC2998 cell growth in a cell viability assay.
|
Homo sapiens
|
6.592
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCC38 cell growth in a cell viability assay.
|
Homo sapiens
|
31.24
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCE-4 cell growth in a cell viability assay.
|
Homo sapiens
|
453.16
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HCT-15 cell growth in a cell viability assay.
|
Homo sapiens
|
95.1
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HD-MY-Z cell growth in a cell viability assay.
|
Homo sapiens
|
560.2
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HMV-II cell growth in a cell viability assay.
|
Homo sapiens
|
69.74
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HOP-62 cell growth in a cell viability assay.
|
Homo sapiens
|
4.134
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HOS cell growth in a cell viability assay.
|
Homo sapiens
|
560.23
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HSC-3 cell growth in a cell viability assay.
|
Homo sapiens
|
688.29
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HT-1080 cell growth in a cell viability assay.
|
Homo sapiens
|
233.57
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HT-144 cell growth in a cell viability assay.
|
Homo sapiens
|
55.14
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HT-29 cell growth in a cell viability assay.
|
Homo sapiens
|
535.5
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human HUTU-80 cell growth in a cell viability assay.
|
Homo sapiens
|
0.1358
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human IGROV-1 cell growth in a cell viability assay.
|
Homo sapiens
|
144.55
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human IMR-5 cell growth in a cell viability assay.
|
Homo sapiens
|
137.36
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human IST-MEL1 cell growth in a cell viability assay.
|
Homo sapiens
|
279.75
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human IST-SL2 cell growth in a cell viability assay.
|
Homo sapiens
|
0.1732
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay.
|
Homo sapiens
|
712.28
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human J82 cell growth in a cell viability assay.
|
Homo sapiens
|
774.31
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human JVM-2 cell growth in a cell viability assay.
|
Homo sapiens
|
572.24
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human KG-1 cell growth in a cell viability assay.
|
Homo sapiens
|
130.57
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human KGN cell growth in a cell viability assay.
|
Homo sapiens
|
3.712
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human KS-1 cell growth in a cell viability assay.
|
Homo sapiens
|
10.84
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human KYSE-150 cell growth in a cell viability assay.
|
Homo sapiens
|
2.647
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human KYSE-270 cell growth in a cell viability assay.
|
Homo sapiens
|
716.9
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LB1047-RCC cell growth in a cell viability assay.
|
Homo sapiens
|
32.55
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LB2241-RCC cell growth in a cell viability assay.
|
Homo sapiens
|
738.25
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LB2518-MEL cell growth in a cell viability assay.
|
Homo sapiens
|
182.25
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LB996-RCC cell growth in a cell viability assay.
|
Homo sapiens
|
175.34
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LC-2-ad cell growth in a cell viability assay.
|
Homo sapiens
|
80.36
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LCLC-103H cell growth in a cell viability assay.
|
Homo sapiens
|
143.98
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LOUCY cell growth in a cell viability assay.
|
Homo sapiens
|
9.935
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LOXIMVI cell growth in a cell viability assay.
|
Homo sapiens
|
452.32
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LS-411N cell growth in a cell viability assay.
|
Homo sapiens
|
52.76
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LU-99A cell growth in a cell viability assay.
|
Homo sapiens
|
4.22
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LXF-289 cell growth in a cell viability assay.
|
Homo sapiens
|
644.25
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human LoVo cell growth in a cell viability assay.
|
Homo sapiens
|
71.17
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MDA-MB-231 cell growth in a cell viability assay.
|
Homo sapiens
|
273.07
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MDA-MB-361 cell growth in a cell viability assay.
|
Homo sapiens
|
719.09
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MEG-01 cell growth in a cell viability assay.
|
Homo sapiens
|
395.49
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MEL-HO cell growth in a cell viability assay.
|
Homo sapiens
|
850.21
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MEL-JUSO cell growth in a cell viability assay.
|
Homo sapiens
|
108.55
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MFE-296 cell growth in a cell viability assay.
|
Homo sapiens
|
153.24
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MFH-ino cell growth in a cell viability assay.
|
Homo sapiens
|
2.646
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MHH-CALL-2 cell growth in a cell viability assay.
|
Homo sapiens
|
534.64
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MHH-ES-1 cell growth in a cell viability assay.
|
Homo sapiens
|
43.57
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay.
|
Homo sapiens
|
110.74
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MKN1 cell growth in a cell viability assay.
|
Homo sapiens
|
79.65
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MKN28 cell growth in a cell viability assay.
|
Homo sapiens
|
1.08
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MKN45 cell growth in a cell viability assay.
|
Homo sapiens
|
24.81
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human ML-2 cell growth in a cell viability assay.
|
Homo sapiens
|
131.66
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MLMA cell growth in a cell viability assay.
|
Homo sapiens
|
870.48
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MV-4-11 cell growth in a cell viability assay.
|
Homo sapiens
|
9.908
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MZ1-PC cell growth in a cell viability assay.
|
Homo sapiens
|
224.34
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human MZ7-mel cell growth in a cell viability assay.
|
Homo sapiens
|
130.5
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NALM-6 cell growth in a cell viability assay.
|
Homo sapiens
|
420.16
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NB69 cell growth in a cell viability assay.
|
Homo sapiens
|
922.54
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H1299 cell growth in a cell viability assay.
|
Homo sapiens
|
107.53
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
SANGER: Inhibition of human NCI-H1437 cell growth in a cell viability assay.
|
Homo sapiens
|
742.72
nM
|
|
Title : Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
|
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) at 20uM using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis
|
Homo sapiens
|
97.5
%
|
|
Journal : Bioorg Med Chem
Title : Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase.
Year : 2020
Volume : 28
Issue : 20.0
First Page : 115675
Last Page : 115675
Authors : Brewitz L,Tumber A,Zhang X,Schofield CJ
Abstract : Human aspartate/asparagine-β-hydroxylase (AspH) is a 2-oxoglutarate (2OG) dependent oxygenase that catalyses the hydroxylation of Asp/Asn-residues of epidermal growth factor-like domains (EGFDs). AspH is reported to be upregulated on the cell surface of invasive cancer cells in a manner distinguishing healthy from cancer cells. We report studies on the effect of small-molecule active pharmaceutical ingredients (APIs) of human cancer therapeutics on the catalytic activity of AspH using a high-throughput mass spectrometry (MS)-based inhibition assay. Human B-cell lymphoma-2 (Bcl-2)-protein inhibitors, including the (R)-enantiomer of the natural product gossypol, were observed to efficiently inhibit AspH, as does the antitumor antibiotic bleomycin A. The results may help in the design of AspH inhibitors with the potential of increased selectivity compared to the previously identified Fe(II)-chelating or 2OG-competitive inhibitors. With regard to the clinical use of bleomycin A and of the Bcl-2 inhibitor venetoclax, the results suggest that possible side-effects mediated through the inhibition of AspH and other 2OG oxygenases should be considered.
