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Assay Detail

CHEMBL4839006

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant FAK (unknown origin) by radiometric kinase assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Focal adhesion kinase 1 (CHEMBL2695)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Thieno[3,2-<i>d</i>]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3.
Cho H, Shin I, Yoon H, Jeon E, Lee J, Kim Y, Ryu S, Song C, Kwon NH, Moon Y, Kim S, Kim ND, Choi HG, Sim T.
J Med Chem (2021) 64 : 11934 -11957
PubMed 34324343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.29 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4851157 1 8.15
CHEMBL4846921 1 8.15
CHEMBL4873104 1 8.10
CHEMBL4846553 1 8.00
CHEMBL4874196 1 7.96
CHEMBL4877875 1 7.92
CHEMBL4854620 1 7.92
CHEMBL4853724 1 7.92
CHEMBL4857298 1 7.89
CHEMBL4846093 1 7.82
CHEMBL4872520 1 7.80
CHEMBL4878656 1 7.75
CHEMBL4849384 1 7.75
CHEMBL4861088 1 7.75
CHEMBL4861397 1 7.68
CHEMBL4862392 1 7.68
CHEMBL4858365 1 7.58
CHEMBL4860735 1 7.54
CHEMBL4871809 1 7.52
CHEMBL4867151 1 7.51
CHEMBL4867910 1 7.48
CHEMBL4877120 1 7.46
CHEMBL4861021 1 7.44
CHEMBL4876873 1 7.31
CHEMBL4876098 1 7.27
CHEMBL4879263 1 7.26
CHEMBL4873271 1 7.23
CHEMBL4874015 1 7.17
CHEMBL4869934 1 7.11
CHEMBL4874892 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4851157 IC50 = 7.0 nM 8.15
CHEMBL4846921 IC50 = 7.0 nM 8.15
CHEMBL4873104 IC50 = 8.0 nM 8.10
CHEMBL4846553 IC50 = 10.0 nM 8.00
CHEMBL4874196 IC50 = 11.0 nM 7.96
CHEMBL4877875 IC50 = 12.0 nM 7.92
CHEMBL4854620 IC50 = 12.0 nM 7.92
CHEMBL4853724 IC50 = 12.0 nM 7.92
CHEMBL4857298 IC50 = 13.0 nM 7.89
CHEMBL4846093 IC50 = 15.0 nM 7.82
CHEMBL4872520 IC50 = 16.0 nM 7.80
CHEMBL4849384 IC50 = 18.0 nM 7.75
CHEMBL4861088 IC50 = 18.0 nM 7.75
CHEMBL4878656 IC50 = 18.0 nM 7.75
CHEMBL4862392 IC50 = 21.0 nM 7.68
CHEMBL4861397 IC50 = 21.0 nM 7.68
CHEMBL4858365 IC50 = 26.0 nM 7.58
CHEMBL4860735 IC50 = 29.0 nM 7.54
CHEMBL4871809 IC50 = 30.0 nM 7.52
CHEMBL4867151 IC50 = 31.0 nM 7.51
CHEMBL4867910 IC50 = 33.0 nM 7.48
CHEMBL4877120 IC50 = 35.0 nM 7.46
CHEMBL4861021 IC50 = 36.0 nM 7.44
CHEMBL4876873 IC50 = 49.0 nM 7.31
CHEMBL4876098 IC50 = 54.0 nM 7.27
CHEMBL4879263 IC50 = 55.0 nM 7.26
CHEMBL4873271 IC50 = 59.0 nM 7.23
CHEMBL4874015 IC50 = 68.0 nM 7.17
CHEMBL4869934 IC50 = 78.0 nM 7.11
CHEMBL4874892 IC50 = 91.0 nM 7.04
CHEMBL4879025 IC50 = 126.0 nM 6.90
CHEMBL4878892 IC50 = 194.0 nM 6.71
CHEMBL205098 IC50 = 200.0 nM 6.70
CHEMBL4867693 IC50 = 321.0 nM 6.49
CHEMBL4849868 IC50 = 361.0 nM 6.44
CHEMBL4850705 IC50 = 668.0 nM 6.17
CHEMBL4878530 IC50 = 717.0 nM 6.14
CHEMBL4878440 IC50 = 1645.0 nM 5.78
CHEMBL4868316 IC50 = 2355.0 nM 5.63
CHEMBL4858147 IC50 = 4032.0 nM 5.39
CHEMBL4855302 IC50 > 10000.0 nM -
CHEMBL3137331 DEFACTINIB IC50 < 0.5 nM -