Synonyms
Status
Molecule Category UNKNOWN
UNII W9E3353E8J

Structure

InChI Key LQVXSNNAFNGRAH-QHCPKHFHSA-N
Smiles C[C@@]1(C(=O)Nc2ccc(F)nc2)CCCN1c1nc(Nc2cc(C3CC3)n[nH]2)c2cccn2n1
InChI
InChI=1S/C23H24FN9O/c1-23(21(34)26-15-7-8-18(24)25-13-15)9-3-10-32(23)22-28-20(17-4-2-11-33(17)31-22)27-19-12-16(29-30-19)14-5-6-14/h2,4,7-8,11-14H,3,5-6,9-10H2,1H3,(H,26,34)(H2,27,28,29,30,31)/t23-/m0/s1

Physicochemical Descriptors

Property Name Value
Molecular Formula C23H24FN9O
Molecular Weight 461.51
AlogP 3.61
Hydrogen Bond Acceptor 8.0
Hydrogen Bond Donor 3.0
Number of Rotational Bond 6.0
Polar Surface Area 116.13
Molecular species NEUTRAL
Aromatic Rings 4.0
Heavy Atoms 34.0

Bioactivity

Mechanism of Action Action Reference
Insulin receptor inhibitor INHIBITOR PubMed PubMed
Protein: Insulin receptor

Description: Insulin receptor

Organism : Homo sapiens

P06213 ENSG00000171105
Protein: Insulin-like growth factor I receptor

Description: Insulin-like growth factor 1 receptor

Organism : Homo sapiens

P08069 ENSG00000140443
Assay Description Organism Bioactivity Reference
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 %

Cross References

Resources Reference
ChEBI 88339
ChEMBL CHEMBL575448
DrugBank DB15399
FDA SRS W9E3353E8J
Guide to Pharmacology 7952
PDB EBI
PubChem 24785538
SureChEMBL SCHEMBL1810808
ZINC ZINC000043203317