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Assay Detail

CHEMBL870124

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

Binding
Inhibition of FAK
77
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Choi HS, Wang Z, Richmond W, He X, Yang K, Jiang T, Karanewsky D, Gu XJ, Zhou V, Liu Y, Che J, Lee CC, Caldwell J, Kanazawa T, Umemura I, Matsuura N, Ohmori O, Honda T, Gray N, He Y.
Bioorg Med Chem Lett (2006) 16 : 2689 -2692
PubMed 16524731 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 77 6.34 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207491 1 8.40
CHEMBL207084 1 7.54
CHEMBL207605 1 7.46
CHEMBL206255 1 7.43
CHEMBL379837 1 7.42
CHEMBL207131 1 7.42
CHEMBL207961 1 7.27
CHEMBL382354 1 7.20
CHEMBL207499 1 7.20
CHEMBL377708 1 7.14
CHEMBL206524 1 7.03
CHEMBL208419 1 6.94
CHEMBL439154 1 6.93
CHEMBL209044 1 6.92
CHEMBL207015 1 6.90
CHEMBL208370 1 6.74
CHEMBL205098 1 6.67
CHEMBL207614 1 6.66
CHEMBL204686 1 6.63
CHEMBL207737 1 6.63
CHEMBL206876 1 6.63
CHEMBL380312 1 6.62
CHEMBL380515 1 6.58
CHEMBL380226 1 6.56
CHEMBL207444 1 6.53
CHEMBL380683 1 6.50
CHEMBL208468 1 6.49
CHEMBL207126 1 6.48
CHEMBL208939 1 6.47
CHEMBL382192 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207491 IC50 = 4.0 nM 8.40
CHEMBL207084 IC50 = 29.0 nM 7.54
CHEMBL207605 IC50 = 35.0 nM 7.46
CHEMBL206255 IC50 = 37.0 nM 7.43
CHEMBL379837 IC50 = 38.0 nM 7.42
CHEMBL207131 IC50 = 38.0 nM 7.42
CHEMBL207961 IC50 = 54.0 nM 7.27
CHEMBL382354 IC50 = 63.0 nM 7.20
CHEMBL207499 IC50 = 63.0 nM 7.20
CHEMBL377708 IC50 = 73.0 nM 7.14
CHEMBL206524 IC50 = 93.0 nM 7.03
CHEMBL208419 IC50 = 115.0 nM 6.94
CHEMBL439154 IC50 = 117.0 nM 6.93
CHEMBL209044 IC50 = 119.0 nM 6.92
CHEMBL207015 IC50 = 126.0 nM 6.90
CHEMBL208370 IC50 = 182.0 nM 6.74
CHEMBL205098 IC50 = 212.0 nM 6.67
CHEMBL207614 IC50 = 221.0 nM 6.66
CHEMBL204686 IC50 = 236.0 nM 6.63
CHEMBL207737 IC50 = 235.0 nM 6.63
CHEMBL206876 IC50 = 232.0 nM 6.63
CHEMBL380312 IC50 = 242.0 nM 6.62
CHEMBL380515 IC50 = 262.0 nM 6.58
CHEMBL380226 IC50 = 278.0 nM 6.56
CHEMBL207444 IC50 = 298.0 nM 6.53
CHEMBL380683 IC50 = 314.0 nM 6.50
CHEMBL208468 IC50 = 322.0 nM 6.49
CHEMBL207126 IC50 = 331.0 nM 6.48
CHEMBL208939 IC50 = 342.0 nM 6.47
CHEMBL382192 IC50 = 339.0 nM 6.47
CHEMBL207259 IC50 = 345.0 nM 6.46
CHEMBL378661 IC50 = 365.0 nM 6.44
CHEMBL208384 IC50 = 397.0 nM 6.40
CHEMBL207721 IC50 = 421.0 nM 6.38
CHEMBL379279 IC50 = 434.0 nM 6.36
CHEMBL206731 IC50 = 504.0 nM 6.30
CHEMBL208368 IC50 = 507.0 nM 6.29
CHEMBL206927 IC50 = 544.0 nM 6.26
CHEMBL207232 IC50 = 635.0 nM 6.20
CHEMBL425418 IC50 = 634.0 nM 6.20
CHEMBL207834 IC50 = 727.0 nM 6.14
CHEMBL208734 IC50 = 727.0 nM 6.14
CHEMBL379655 IC50 = 831.0 nM 6.08
CHEMBL380424 IC50 = 882.0 nM 6.05
CHEMBL208000 IC50 = 983.0 nM 6.01
CHEMBL379969 IC50 = 1330.0 nM 5.88
CHEMBL207053 IC50 = 1510.0 nM 5.82
CHEMBL381374 IC50 = 1507.0 nM 5.82
CHEMBL381262 IC50 = 1530.0 nM 5.82
CHEMBL383263 IC50 = 1810.0 nM 5.74