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Assay Detail

CHEMBL1825352

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Binding
Binding affinity to human recombinant c-MET assessed as inhibition of autophosphorylation by continuous fluorometric assay
ChEMBL ↗
44
Total Activities
44
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

Hepatocyte growth factor receptor (CHEMBL3717) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I, McTigue M, Grodsky N, Ryan K, Padrique E, Alton G, Timofeevski S, Yamazaki S, Li Q, Zou H, Christensen J, Mroczkowski B, Bender S, Kania RS, Edwards MP.
J Med Chem (2011) 54 : 6342 -6363
PubMed 21812414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.56 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL601719 CRIZOTINIB 4.0 1 8.70
CHEMBL1824878 — — 1 7.92
CHEMBL1825136 — — 1 7.85
CHEMBL1825138 — — 1 7.71
CHEMBL1825133 — — 1 7.62
CHEMBL1825135 — — 1 7.58
CHEMBL1824884 — — 1 7.46
CHEMBL1825134 — — 1 7.45
CHEMBL1821759 — — 1 7.43
CHEMBL1825137 — — 1 7.42
CHEMBL1824886 — — 1 7.39
CHEMBL1825131 — — 1 7.34
CHEMBL1824894 — — 1 7.34
CHEMBL1825130 — — 1 7.31
CHEMBL1824895 — — 1 7.22
CHEMBL1824877 — — 1 7.17
CHEMBL1825132 — — 1 7.15
CHEMBL1824885 — — 1 7.12
CHEMBL1824892 — — 1 7.09
CHEMBL1825141 — — 1 6.79
CHEMBL1824890 — — 1 6.70
CHEMBL1824893 — — 1 6.64
CHEMBL1824888 — — 1 6.62
CHEMBL1824876 — — 1 6.58
CHEMBL1824891 — — 1 6.46
CHEMBL1824866 — — 1 6.34
CHEMBL1824889 — — 1 6.11
CHEMBL1824875 — — 1 6.06
CHEMBL1824872 — — 1 6.01
CHEMBL1824883 — — 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL601719 CRIZOTINIB Ki = 2.0 nM 8.70
CHEMBL1824878 — Ki = 12.0 nM 7.92
CHEMBL1825136 — Ki = 14.0 nM 7.85
CHEMBL1825138 — Ki = 19.3 nM 7.71
CHEMBL1825133 — Ki = 23.7 nM 7.62
CHEMBL1825135 — Ki = 26.0 nM 7.58
CHEMBL1824884 — Ki = 35.0 nM 7.46
CHEMBL1825134 — Ki = 35.2 nM 7.45
CHEMBL1821759 — Ki = 37.1 nM 7.43
CHEMBL1825137 — Ki = 38.3 nM 7.42
CHEMBL1824886 — Ki = 41.1 nM 7.39
CHEMBL1824894 — Ki = 46.0 nM 7.34
CHEMBL1825131 — Ki = 45.7 nM 7.34
CHEMBL1825130 — Ki = 48.6 nM 7.31
CHEMBL1824895 — Ki = 59.7 nM 7.22
CHEMBL1824877 — Ki = 68.0 nM 7.17
CHEMBL1825132 — Ki = 70.2 nM 7.15
CHEMBL1824885 — Ki = 75.0 nM 7.12
CHEMBL1824892 — Ki = 81.5 nM 7.09
CHEMBL1825141 — Ki = 161.0 nM 6.79
CHEMBL1824890 — Ki = 201.0 nM 6.70
CHEMBL1824893 — Ki = 230.0 nM 6.64
CHEMBL1824888 — Ki = 240.0 nM 6.62
CHEMBL1824876 — Ki = 260.0 nM 6.58
CHEMBL1824891 — Ki = 348.0 nM 6.46
CHEMBL1824866 — Ki = 460.0 nM 6.34
CHEMBL1824889 — Ki = 780.0 nM 6.11
CHEMBL1824875 — Ki = 880.0 nM 6.06
CHEMBL1824872 — Ki = 980.0 nM 6.01
CHEMBL1824883 — Ki = 1020.0 nM 5.99
CHEMBL1824873 — Ki = 1030.0 nM 5.99
CHEMBL1824869 — Ki = 1710.0 nM 5.77
CHEMBL1824882 — Ki = 1980.0 nM 5.70
CHEMBL1825140 — Ki = 2450.0 nM 5.61
CHEMBL1824871 — Ki = 2590.0 nM 5.59
CHEMBL1824868 — Ki = 2820.0 nM 5.55
CHEMBL1824887 — Ki = 3190.0 nM 5.50
CHEMBL1825139 — Ki = 3830.0 nM 5.42
CHEMBL1824874 — Ki = 5110.0 nM 5.29
CHEMBL1824870 — Ki = 6500.0 nM 5.19
CHEMBL1824880 — Ki = 6560.0 nM 5.18
CHEMBL1824879 — Ki = 7230.0 nM 5.14
CHEMBL1824881 — Ki = 7580.0 nM 5.12
CHEMBL1824867 — Ki = 7920.0 nM 5.10