Inhibition of IGF1R after 60 mins by fluorescence electrophoresis
|
None
|
2.0
nM
|
|
Antiproliferative activity against mouse Sal cells overexpressing IGF1R assessed as [3H]thymidine incorporation into DNA after 72 hrs
|
Mus musculus
|
7.0
nM
|
|
Inhibition of IGF1R phosphorylation in mouse Sal cells by Western blotting
|
Mus musculus
|
13.0
nM
|
|
Inhibition of Akt phosphorylation in mouse Sal cells by Western blotting
|
Mus musculus
|
22.0
nM
|
|
Inhibition of MAPK phosphorylation in mouse Sal cells by Western blotting
|
Mus musculus
|
13.0
nM
|
|
Inhibition of IGF1R
|
None
|
8.4
nM
|
|
Inhibition of IGF1R in IGF1R-SAL cells
|
None
|
2.1
nM
|
|
SANGER: Inhibition of human NCI-H1618 cell growth in a cell viability assay.
|
Homo sapiens
|
739.03
nM
|
|
SANGER: Inhibition of human NCI-H1648 cell growth in a cell viability assay.
|
Homo sapiens
|
160.75
nM
|
|
SANGER: Inhibition of human NCI-H1651 cell growth in a cell viability assay.
|
Homo sapiens
|
801.82
nM
|
|
SANGER: Inhibition of human NCI-H1734 cell growth in a cell viability assay.
|
Homo sapiens
|
762.9
nM
|
|
SANGER: Inhibition of human NCI-H1770 cell growth in a cell viability assay.
|
Homo sapiens
|
674.03
nM
|
|
SANGER: Inhibition of human NCI-H1882 cell growth in a cell viability assay.
|
Homo sapiens
|
810.14
nM
|
|
SANGER: Inhibition of human NCI-H2122 cell growth in a cell viability assay.
|
Homo sapiens
|
14.58
nM
|
|
SANGER: Inhibition of human NCI-H2141 cell growth in a cell viability assay.
|
Homo sapiens
|
698.19
nM
|
|
SANGER: Inhibition of human NCI-H2171 cell growth in a cell viability assay.
|
Homo sapiens
|
411.71
nM
|
|
SANGER: Inhibition of human NCI-H2228 cell growth in a cell viability assay.
|
Homo sapiens
|
124.27
nM
|
|
SANGER: Inhibition of human NCI-H2342 cell growth in a cell viability assay.
|
Homo sapiens
|
728.29
nM
|
|
SANGER: Inhibition of human NCI-H292 cell growth in a cell viability assay.
|
Homo sapiens
|
369.62
nM
|
|
SANGER: Inhibition of human NCI-H358 cell growth in a cell viability assay.
|
Homo sapiens
|
55.71
nM
|
|
SANGER: Inhibition of human NCI-H441 cell growth in a cell viability assay.
|
Homo sapiens
|
353.95
nM
|
|
SANGER: Inhibition of human NCI-H650 cell growth in a cell viability assay.
|
Homo sapiens
|
26.52
nM
|
|
SANGER: Inhibition of human NCI-H727 cell growth in a cell viability assay.
|
Homo sapiens
|
30.11
nM
|
|
SANGER: Inhibition of human NCI-H747 cell growth in a cell viability assay.
|
Homo sapiens
|
199.05
nM
|
|
SANGER: Inhibition of human NCI-H810 cell growth in a cell viability assay.
|
Homo sapiens
|
137.07
nM
|
|
SANGER: Inhibition of human NH-12 cell growth in a cell viability assay.
|
Homo sapiens
|
179.43
nM
|
|
SANGER: Inhibition of human NMC-G1 cell growth in a cell viability assay.
|
Homo sapiens
|
208.52
nM
|
|
SANGER: Inhibition of human NOS-1 cell growth in a cell viability assay.
|
Homo sapiens
|
30.84
nM
|
|
SANGER: Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.
|
Homo sapiens
|
177.78
nM
|
|
SANGER: Inhibition of human OPM-2 cell growth in a cell viability assay.
|
Homo sapiens
|
611.61
nM
|
|
SANGER: Inhibition of human OVCAR-5 cell growth in a cell viability assay.
|
Homo sapiens
|
502.07
nM
|
|
SANGER: Inhibition of human PANC-08-13 cell growth in a cell viability assay.
|
Homo sapiens
|
8.604
nM
|
|
SANGER: Inhibition of human PANC-10-05 cell growth in a cell viability assay.
|
Homo sapiens
|
217.13
nM
|
|
SANGER: Inhibition of human PSN1 cell growth in a cell viability assay.
|
Homo sapiens
|
78.22
nM
|
|
SANGER: Inhibition of human RD cell growth in a cell viability assay.
|
Homo sapiens
|
185.31
nM
|
|
SANGER: Inhibition of human RH-1 cell growth in a cell viability assay.
|
Homo sapiens
|
166.29
nM
|
|
SANGER: Inhibition of human RPMI-2650 cell growth in a cell viability assay.
|
Homo sapiens
|
175.67
nM
|
|
SANGER: Inhibition of human RS4-11 cell growth in a cell viability assay.
|
Homo sapiens
|
102.4
nM
|
|
SANGER: Inhibition of human RT-112 cell growth in a cell viability assay.
|
Homo sapiens
|
751.08
nM
|
|
SANGER: Inhibition of human SBC-5 cell growth in a cell viability assay.
|
Homo sapiens
|
470.41
nM
|
|
SANGER: Inhibition of human SCC-4 cell growth in a cell viability assay.
|
Homo sapiens
|
786.76
nM
|
|
SANGER: Inhibition of human SIG-M5 cell growth in a cell viability assay.
|
Homo sapiens
|
48.19
nM
|
|
SANGER: Inhibition of human SIMA cell growth in a cell viability assay.
|
Homo sapiens
|
340.69
nM
|
|
SANGER: Inhibition of human SJRH30 cell growth in a cell viability assay.
|
Homo sapiens
|
109.82
nM
|
|
SANGER: Inhibition of human SJSA-1 cell growth in a cell viability assay.
|
Homo sapiens
|
326.1
nM
|
|
SANGER: Inhibition of human SK-CO-1 cell growth in a cell viability assay.
|
Homo sapiens
|
197.24
nM
|
|
SANGER: Inhibition of human SK-LU-1 cell growth in a cell viability assay.
|
Homo sapiens
|
243.3
nM
|
|
SANGER: Inhibition of human SK-MEL-2 cell growth in a cell viability assay.
|
Homo sapiens
|
418.05
nM
|
|
SANGER: Inhibition of human SK-MEL-3 cell growth in a cell viability assay.
|
Homo sapiens
|
258.34
nM
|
|
SANGER: Inhibition of human SK-MM-2 cell growth in a cell viability assay.
|
Homo sapiens
|
395.16
nM
|
|
SANGER: Inhibition of human SK-N-DZ cell growth in a cell viability assay.
|
Homo sapiens
|
77.92
nM
|
|
SANGER: Inhibition of human SK-NEP-1 cell growth in a cell viability assay.
|
Homo sapiens
|
228.35
nM
|
|
SANGER: Inhibition of human SK-OV-3 cell growth in a cell viability assay.
|
Homo sapiens
|
712.64
nM
|
|
SANGER: Inhibition of human SK-PN-DW cell growth in a cell viability assay.
|
Homo sapiens
|
227.86
nM
|
|
SANGER: Inhibition of human SNB75 cell growth in a cell viability assay.
|
Homo sapiens
|
673.77
nM
|
|
SANGER: Inhibition of human SNG-M cell growth in a cell viability assay.
|
Homo sapiens
|
783.94
nM
|
|
SANGER: Inhibition of human SNU-387 cell growth in a cell viability assay.
|
Homo sapiens
|
35.78
nM
|
|
SANGER: Inhibition of human SNU-C1 cell growth in a cell viability assay.
|
Homo sapiens
|
86.17
nM
|
|
SANGER: Inhibition of human SW1710 cell growth in a cell viability assay.
|
Homo sapiens
|
216.0
nM
|
|
SANGER: Inhibition of human SW48 cell growth in a cell viability assay.
|
Homo sapiens
|
749.63
nM
|
|
SANGER: Inhibition of human SW620 cell growth in a cell viability assay.
|
Homo sapiens
|
807.13
nM
|
|
SANGER: Inhibition of human SW872 cell growth in a cell viability assay.
|
Homo sapiens
|
993.24
nM
|
|
SANGER: Inhibition of human SW948 cell growth in a cell viability assay.
|
Homo sapiens
|
692.6
nM
|
|
SANGER: Inhibition of human SW954 cell growth in a cell viability assay.
|
Homo sapiens
|
793.03
nM
|
|
SANGER: Inhibition of human SW982 cell growth in a cell viability assay.
|
Homo sapiens
|
478.69
nM
|
|
SANGER: Inhibition of human Saos-2 cell growth in a cell viability assay.
|
Homo sapiens
|
9.62
nM
|
|
SANGER: Inhibition of human T84 cell growth in a cell viability assay.
|
Homo sapiens
|
33.59
nM
|
|
SANGER: Inhibition of human TCCSUP cell growth in a cell viability assay.
|
Homo sapiens
|
430.88
nM
|
|
SANGER: Inhibition of human TE-1 cell growth in a cell viability assay.
|
Homo sapiens
|
549.63
nM
|
|
SANGER: Inhibition of human 5637 cell growth in a cell viability assay.
|
Homo sapiens
|
600.92
nM
|
|
SANGER: Inhibition of human 639-V cell growth in a cell viability assay.
|
Homo sapiens
|
990.07
nM
|
|
SANGER: Inhibition of human 786-0 cell growth in a cell viability assay.
|
Homo sapiens
|
969.04
nM
|
|
SANGER: Inhibition of human A101D cell growth in a cell viability assay.
|
Homo sapiens
|
976.46
nM
|
|
SANGER: Inhibition of human A2780 cell growth in a cell viability assay.
|
Homo sapiens
|
863.27
nM
|
|
SANGER: Inhibition of human A375 cell growth in a cell viability assay.
|
Homo sapiens
|
66.78
nM
|
|
SANGER: Inhibition of human A4-Fuk cell growth in a cell viability assay.
|
Homo sapiens
|
5.7
nM
|
|
SANGER: Inhibition of human A427 cell growth in a cell viability assay.
|
Homo sapiens
|
243.22
nM
|
|
SANGER: Inhibition of human A431 cell growth in a cell viability assay.
|
Homo sapiens
|
354.21
nM
|
|
SANGER: Inhibition of human A673 cell growth in a cell viability assay.
|
Homo sapiens
|
604.86
nM
|
|
SANGER: Inhibition of human ABC-1 cell growth in a cell viability assay.
|
Homo sapiens
|
116.95
nM
|
|
SANGER: Inhibition of human AN3-CA cell growth in a cell viability assay.
|
Homo sapiens
|
656.46
nM
|
|
SANGER: Inhibition of human BB30-HNC cell growth in a cell viability assay.
|
Homo sapiens
|
663.81
nM
|
|
SANGER: Inhibition of human BB49-HNC cell growth in a cell viability assay.
|
Homo sapiens
|
477.33
nM
|
|
SANGER: Inhibition of human BC-1 cell growth in a cell viability assay.
|
Homo sapiens
|
587.45
nM
|
|
SANGER: Inhibition of human BCPAP cell growth in a cell viability assay.
|
Homo sapiens
|
877.37
nM
|
|
SANGER: Inhibition of human BFTC-905 cell growth in a cell viability assay.
|
Homo sapiens
|
47.27
nM
|
|
SANGER: Inhibition of human CAL-12T cell growth in a cell viability assay.
|
Homo sapiens
|
372.16
nM
|
|
SANGER: Inhibition of human CAL-39 cell growth in a cell viability assay.
|
Homo sapiens
|
82.59
nM
|
|
SANGER: Inhibition of human CAL-51 cell growth in a cell viability assay.
|
Homo sapiens
|
402.69
nM
|
|
SANGER: Inhibition of human CAL-85-1 cell growth in a cell viability assay.
|
Homo sapiens
|
167.38
nM
|
|
SANGER: Inhibition of human TE-10 cell growth in a cell viability assay.
|
Homo sapiens
|
630.65
nM
|
|
SANGER: Inhibition of human TE-11 cell growth in a cell viability assay.
|
Homo sapiens
|
4.197
nM
|
|
SANGER: Inhibition of human TE-12 cell growth in a cell viability assay.
|
Homo sapiens
|
358.41
nM
|
|
SANGER: Inhibition of human TE-15 cell growth in a cell viability assay.
|
Homo sapiens
|
955.56
nM
|
|
SANGER: Inhibition of human TE-441-T cell growth in a cell viability assay.
|
Homo sapiens
|
563.55
nM
|
|
SANGER: Inhibition of human TE-8 cell growth in a cell viability assay.
|
Homo sapiens
|
36.54
nM
|
|
SANGER: Inhibition of human TGBC24TKB cell growth in a cell viability assay.
|
Homo sapiens
|
357.05
nM
|
|
SANGER: Inhibition of human VA-ES-BJ cell growth in a cell viability assay.
|
Homo sapiens
|
632.47
nM
|
|
SANGER: Inhibition of human YKG-1 cell growth in a cell viability assay.
|
Homo sapiens
|
831.03
nM
|
|
SANGER: Inhibition of human CCF-STTG1 cell growth in a cell viability assay.
|
Homo sapiens
|
513.74
nM
|
|
SANGER: Inhibition of human CHP-126 cell growth in a cell viability assay.
|
Homo sapiens
|
431.02
nM
|
|
SANGER: Inhibition of human CHP-212 cell growth in a cell viability assay.
|
Homo sapiens
|
151.62
nM
|
|
SANGER: Inhibition of human CMK cell growth in a cell viability assay.
|
Homo sapiens
|
92.83
nM
|
|
SANGER: Inhibition of human COLO-205 cell growth in a cell viability assay.
|
Homo sapiens
|
2.243
nM
|
|
SANGER: Inhibition of human COLO-320-HSR cell growth in a cell viability assay.
|
Homo sapiens
|
179.58
nM
|
|
SANGER: Inhibition of human COLO-668 cell growth in a cell viability assay.
|
Homo sapiens
|
427.37
nM
|
|
SANGER: Inhibition of human COLO-680N cell growth in a cell viability assay.
|
Homo sapiens
|
799.45
nM
|
|
SANGER: Inhibition of human COR-L105 cell growth in a cell viability assay.
|
Homo sapiens
|
132.32
nM
|
|
SANGER: Inhibition of human COR-L23 cell growth in a cell viability assay.
|
Homo sapiens
|
965.3
nM
|
|
SANGER: Inhibition of human CPC-N cell growth in a cell viability assay.
|
Homo sapiens
|
555.98
nM
|
|
SANGER: Inhibition of human Capan-2 cell growth in a cell viability assay.
|
Homo sapiens
|
206.35
nM
|
|
SANGER: Inhibition of human DK-MG cell growth in a cell viability assay.
|
Homo sapiens
|
617.51
nM
|
|
SANGER: Inhibition of human DMS-273 cell growth in a cell viability assay.
|
Homo sapiens
|
741.75
nM
|
|
SANGER: Inhibition of human DOK cell growth in a cell viability assay.
|
Homo sapiens
|
194.84
nM
|
|
SANGER: Inhibition of human EKVX cell growth in a cell viability assay.
|
Homo sapiens
|
350.75
nM
|
|
SANGER: Inhibition of human ES1 cell growth in a cell viability assay.
|
Homo sapiens
|
15.94
nM
|
|
SANGER: Inhibition of human ES3 cell growth in a cell viability assay.
|
Homo sapiens
|
222.85
nM
|
|
SANGER: Inhibition of human ES4 cell growth in a cell viability assay.
|
Homo sapiens
|
72.93
nM
|
|
SANGER: Inhibition of human ES6 cell growth in a cell viability assay.
|
Homo sapiens
|
214.02
nM
|
|
SANGER: Inhibition of human ES8 cell growth in a cell viability assay.
|
Homo sapiens
|
100.16
nM
|
|
SANGER: Inhibition of human EW-1 cell growth in a cell viability assay.
|
Homo sapiens
|
3.998
nM
|
|
SANGER: Inhibition of human EW-11 cell growth in a cell viability assay.
|
Homo sapiens
|
55.8
nM
|
|
SANGER: Inhibition of human EW-13 cell growth in a cell viability assay.
|
Homo sapiens
|
909.0
nM
|
|
SANGER: Inhibition of human EW-16 cell growth in a cell viability assay.
|
Homo sapiens
|
20.95
nM
|
|
SANGER: Inhibition of human EW-18 cell growth in a cell viability assay.
|
Homo sapiens
|
71.57
nM
|
|
SANGER: Inhibition of human EW-7 cell growth in a cell viability assay.
|
Homo sapiens
|
61.01
nM
|
|
SANGER: Inhibition of human G-401 cell growth in a cell viability assay.
|
Homo sapiens
|
67.81
nM
|
|
SANGER: Inhibition of human G-402 cell growth in a cell viability assay.
|
Homo sapiens
|
978.55
nM
|
|
SANGER: Inhibition of human GB-1 cell growth in a cell viability assay.
|
Homo sapiens
|
362.8
nM
|
|
SANGER: Inhibition of human GCIY cell growth in a cell viability assay.
|
Homo sapiens
|
111.82
nM
|
|
SANGER: Inhibition of human GDM-1 cell growth in a cell viability assay.
|
Homo sapiens
|
53.38
nM
|
|
SANGER: Inhibition of human GI-1 cell growth in a cell viability assay.
|
Homo sapiens
|
725.02
nM
|
|
SANGER: Inhibition of human GI-ME-N cell growth in a cell viability assay.
|
Homo sapiens
|
379.33
nM
|
|
SANGER: Inhibition of human GP5d cell growth in a cell viability assay.
|
Homo sapiens
|
54.04
nM
|
|
SANGER: Inhibition of human H4 cell growth in a cell viability assay.
|
Homo sapiens
|
903.56
nM
|
|
SANGER: Inhibition of human HCC2157 cell growth in a cell viability assay.
|
Homo sapiens
|
356.86
nM
|
|
SANGER: Inhibition of human HCC2998 cell growth in a cell viability assay.
|
Homo sapiens
|
71.9
nM
|
|
SANGER: Inhibition of human HCC70 cell growth in a cell viability assay.
|
Homo sapiens
|
284.48
nM
|
|
SANGER: Inhibition of human HGC-27 cell growth in a cell viability assay.
|
Homo sapiens
|
623.79
nM
|
|
SANGER: Inhibition of human HMV-II cell growth in a cell viability assay.
|
Homo sapiens
|
183.25
nM
|
|
SANGER: Inhibition of human HSC-2 cell growth in a cell viability assay.
|
Homo sapiens
|
910.76
nM
|
|
SANGER: Inhibition of human HSC-3 cell growth in a cell viability assay.
|
Homo sapiens
|
668.43
nM
|
|
SANGER: Inhibition of human HT-144 cell growth in a cell viability assay.
|
Homo sapiens
|
37.91
nM
|
|
SANGER: Inhibition of human HT-29 cell growth in a cell viability assay.
|
Homo sapiens
|
12.26
nM
|
|
SANGER: Inhibition of human HUTU-80 cell growth in a cell viability assay.
|
Homo sapiens
|
278.84
nM
|
|
SANGER: Inhibition of human IGROV-1 cell growth in a cell viability assay.
|
Homo sapiens
|
68.57
nM
|
|
SANGER: Inhibition of human KGN cell growth in a cell viability assay.
|
Homo sapiens
|
558.92
nM
|
|
SANGER: Inhibition of human KM12 cell growth in a cell viability assay.
|
Homo sapiens
|
57.22
nM
|
|
SANGER: Inhibition of human KOSC-2 cell growth in a cell viability assay.
|
Homo sapiens
|
637.21
nM
|
|
SANGER: Inhibition of human KS-1 cell growth in a cell viability assay.
|
Homo sapiens
|
15.94
nM
|
|
SANGER: Inhibition of human KYSE-270 cell growth in a cell viability assay.
|
Homo sapiens
|
809.89
nM
|
|
SANGER: Inhibition of human KYSE-510 cell growth in a cell viability assay.
|
Homo sapiens
|
517.55
nM
|
|
SANGER: Inhibition of human L-363 cell growth in a cell viability assay.
|
Homo sapiens
|
387.03
nM
|
|
SANGER: Inhibition of human LAN-6 cell growth in a cell viability assay.
|
Homo sapiens
|
198.76
nM
|
|
SANGER: Inhibition of human LB1047-RCC cell growth in a cell viability assay.
|
Homo sapiens
|
643.57
nM
|
|
SANGER: Inhibition of human LB647-SCLC cell growth in a cell viability assay.
|
Homo sapiens
|
154.9
nM
|
|
SANGER: Inhibition of human LB771-HNC cell growth in a cell viability assay.
|
Homo sapiens
|
22.96
nM
|
|
SANGER: Inhibition of human LB996-RCC cell growth in a cell viability assay.
|
Homo sapiens
|
562.24
nM
|
|
SANGER: Inhibition of human LC-2-ad cell growth in a cell viability assay.
|
Homo sapiens
|
270.37
nM
|
|
SANGER: Inhibition of human LCLC-103H cell growth in a cell viability assay.
|
Homo sapiens
|
788.34
nM
|
|
SANGER: Inhibition of human LCLC-97TM1 cell growth in a cell viability assay.
|
Homo sapiens
|
43.54
nM
|
|
SANGER: Inhibition of human LK-2 cell growth in a cell viability assay.
|
Homo sapiens
|
341.24
nM
|
|
SANGER: Inhibition of human LS-1034 cell growth in a cell viability assay.
|
Homo sapiens
|
46.06
nM
|
|
SANGER: Inhibition of human LS-411N cell growth in a cell viability assay.
|
Homo sapiens
|
183.49
nM
|
|
SANGER: Inhibition of human LS-513 cell growth in a cell viability assay.
|
Homo sapiens
|
785.87
nM
|
|
SANGER: Inhibition of human LU-99A cell growth in a cell viability assay.
|
Homo sapiens
|
446.55
nM
|
|
SANGER: Inhibition of human MC-IXC cell growth in a cell viability assay.
|
Homo sapiens
|
179.96
nM
|
|
SANGER: Inhibition of human MCF7 cell growth in a cell viability assay.
|
Homo sapiens
|
92.99
nM
|
|
SANGER: Inhibition of human MEL-JUSO cell growth in a cell viability assay.
|
Homo sapiens
|
71.54
nM
|
|
SANGER: Inhibition of human MES-SA cell growth in a cell viability assay.
|
Homo sapiens
|
873.72
nM
|
|
SANGER: Inhibition of human MFH-ino cell growth in a cell viability assay.
|
Homo sapiens
|
71.49
nM
|
|
SANGER: Inhibition of human MG-63 cell growth in a cell viability assay.
|
Homo sapiens
|
276.22
nM
|
|
SANGER: Inhibition of human MHH-ES-1 cell growth in a cell viability assay.
|
Homo sapiens
|
122.06
nM
|
|
SANGER: Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay.
|
Homo sapiens
|
252.62
nM
|
|
SANGER: Inhibition of human MKN45 cell growth in a cell viability assay.
|
Homo sapiens
|
659.87
nM
|
|
SANGER: Inhibition of human ML-2 cell growth in a cell viability assay.
|
Homo sapiens
|
36.95
nM
|
|
SANGER: Inhibition of human MZ1-PC cell growth in a cell viability assay.
|
Homo sapiens
|
215.84
nM
|
|
SANGER: Inhibition of human MZ2-MEL cell growth in a cell viability assay.
|
Homo sapiens
|
998.16
nM
|
|
SANGER: Inhibition of human NB1 cell growth in a cell viability assay.
|
Homo sapiens
|
731.21
nM
|
|
SANGER: Inhibition of human NB10 cell growth in a cell viability assay.
|
Homo sapiens
|
170.84
nM
|
|
SANGER: Inhibition of human NB69 cell growth in a cell viability assay.
|
Homo sapiens
|
363.69
nM
|
|
SANGER: Inhibition of human NCI-H1299 cell growth in a cell viability assay.
|
Homo sapiens
|
648.14
nM
|
|
SANGER: Inhibition of human NCI-H1355 cell growth in a cell viability assay.
|
Homo sapiens
|
14.01
nM
|
|
SANGER: Inhibition of human NCI-H1437 cell growth in a cell viability assay.
|
Homo sapiens
|
105.34
nM
|
|
Tyrosine Kinase Assay: Kinase assay using IGF1-receptor.
|
Homo sapiens
|
2.0
nM
|
|
IGF1R diphosphorilated was immobilized on a Biacore CM5 chip at 25 degrees C with 2uM K04355 and a flow rate of 30 uL/min using amine coupling at pH 4.50 according to Biacore standard protocol. Data sets were processed and analyzed using the software Biacore 4000 Evaluation. Solvent corrected and double-referenced association and dissociation phase data were fitted to a simple 1:1 interaction model with mass transport limitations
|
Homo sapiens
|
0.9615
nM
|
|
Further kinetic evaluation of compounds supplied by Sanofi against AuroraA within a BIAcore3000 instrument
|
Homo sapiens
|
32.74
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
76.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
154.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
799.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
5.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
20.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
14.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
654.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
10.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
865.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
409.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
272.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
11.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
98.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
675.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
152.0
nM
|
|
Inhibition of TRKA (unknown origin)
|
Homo sapiens
|
7.0
nM
|
|
Inhibition of TRKB (unknown origin)
|
Homo sapiens
|
4.0
nM
|
|
Inhibition of IGF-1R (unknown origin)
|
Homo sapiens
|
1.8
nM
|
|
Inhibition of IR (unknown origin)
|
Homo sapiens
|
1.7
nM
|
|
Inhibition of ABCC1 in human H69AR cells at 10 uM preincubated for 30 mins followed by calcein-AM addition measured at 60 secs time interval by fluorescence assay relative to control
|
Homo sapiens
|
20.0
%
|
|
Inhibition of ABCB1 in human A2780/ADR cells at 10 uM preincubated for 30 mins followed by calcein AM addition and measured at 60 secs time interval by fluorescence assay relative to cyclosporine A
|
Homo sapiens
|
20.0
%
|
|
Inhibition of ABCG2 (unknown origin) expressed in MDCK2 cells co-expressing BCRP (unknown origin) assessed as effect on pheophorbide A accumulation at 10 uM pre-incubated for 20 mins followed by pheophorbide A addition and measured after 120 mins by flow cytometric analysis relative to Ko143
|
Homo sapiens
|
20.0
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
13.77
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
6.8
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
1.51
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.71
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.71
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
1.51
%
|
|
Inhibition of INSR (unknown origin) at 1.52 nM relative to control
|
Homo sapiens
|
87.7
%
|
|
Inhibition of IGF1R (unknown origin) at 1.52 nM relative to control
|
Homo sapiens
|
95.0
%
|
|
Inhibition of TRKB (unknown origin) at 1.52 nM relative to control
|
Homo sapiens
|
95.0
%
|
|
Inhibition of MUSK (unknown origin) at 100 nM relative to control
|
Homo sapiens
|
75.1
%
|
|