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Assay Detail

CHEMBL2175489

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Functional
Antagonist activity at c-MET receptor in human A549 cells assessed as inhibition of autophosphorylation after 1 hr by ELISA
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
Cui JJ, McTigue M, Nambu M, Tran-Dubé M, Pairish M, Shen H, Jia L, Cheng H, Hoffman J, Le P, Jalaie M, Goetz GH, Ryan K, Grodsky N, Deng YL, Parker M, Timofeevski S, Murray BW, Yamazaki S, Aguirre S, Li Q, Zou H, Christensen J.
J Med Chem (2012) 55 : 8091 -8109
PubMed 22924734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.36 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170816 — — 1 9.00
CHEMBL2170966 — — 1 8.52
CHEMBL2001019 PF-04217903 1.0 1 8.40
CHEMBL2170967 — — 1 8.30
CHEMBL2170954 — — 1 8.30
CHEMBL2170818 — — 1 8.22
CHEMBL2170969 — — 1 8.15
CHEMBL2170957 — — 1 8.15
CHEMBL2170956 — — 1 8.15
CHEMBL2170806 — — 1 7.85
CHEMBL2170949 — — 1 7.80
CHEMBL2170968 — — 1 7.80
CHEMBL2170947 — — 1 7.80
CHEMBL2170820 — — 1 7.77
CHEMBL2170819 — — 1 7.60
CHEMBL2170808 — — 1 7.60
CHEMBL2170955 — — 1 7.57
CHEMBL2170946 — — 1 7.57
CHEMBL2170950 — — 1 7.48
CHEMBL2170953 — — 1 7.47
CHEMBL2170814 — — 1 7.45
CHEMBL2169896 — — 1 7.32
CHEMBL2170813 — — 1 7.29
CHEMBL2170807 — — 1 7.28
CHEMBL2170952 — — 1 7.09
CHEMBL2170948 — — 1 7.04
CHEMBL2170959 — — 1 6.95
CHEMBL2170810 — — 1 6.85
CHEMBL2170815 — — 1 6.84
CHEMBL2170805 — — 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170816 — IC50 = 1.0 nM 9.00
CHEMBL2170966 — IC50 = 3.0 nM 8.52
CHEMBL2001019 PF-04217903 IC50 = 4.0 nM 8.40
CHEMBL2170967 — IC50 = 5.0 nM 8.30
CHEMBL2170954 — IC50 = 5.0 nM 8.30
CHEMBL2170818 — IC50 = 6.0 nM 8.22
CHEMBL2170969 — IC50 = 7.0 nM 8.15
CHEMBL2170957 — IC50 = 7.0 nM 8.15
CHEMBL2170956 — IC50 = 7.0 nM 8.15
CHEMBL2170806 — IC50 = 14.0 nM 7.85
CHEMBL2170947 — IC50 = 16.0 nM 7.80
CHEMBL2170968 — IC50 = 16.0 nM 7.80
CHEMBL2170949 — IC50 = 16.0 nM 7.80
CHEMBL2170820 — IC50 = 17.0 nM 7.77
CHEMBL2170808 — IC50 = 25.0 nM 7.60
CHEMBL2170819 — IC50 = 25.0 nM 7.60
CHEMBL2170955 — IC50 = 27.0 nM 7.57
CHEMBL2170946 — IC50 = 27.0 nM 7.57
CHEMBL2170950 — IC50 = 33.0 nM 7.48
CHEMBL2170953 — IC50 = 34.0 nM 7.47
CHEMBL2170814 — IC50 = 35.6 nM 7.45
CHEMBL2169896 — IC50 = 48.0 nM 7.32
CHEMBL2170813 — IC50 = 51.0 nM 7.29
CHEMBL2170807 — IC50 = 53.0 nM 7.28
CHEMBL2170952 — IC50 = 82.0 nM 7.09
CHEMBL2170948 — IC50 = 91.0 nM 7.04
CHEMBL2170959 — IC50 = 113.0 nM 6.95
CHEMBL2170810 — IC50 = 141.0 nM 6.85
CHEMBL2170815 — IC50 = 146.0 nM 6.84
CHEMBL2170805 — IC50 = 165.0 nM 6.78
CHEMBL2170809 — IC50 = 166.0 nM 6.78
CHEMBL2170961 — IC50 = 189.0 nM 6.72
CHEMBL2170951 — IC50 = 253.0 nM 6.60
CHEMBL2170965 — IC50 = 520.0 nM 6.28
CHEMBL2170811 — IC50 = 2920.0 nM 5.54
CHEMBL2170962 — IC50 = 10000.0 nM 5.00
CHEMBL2170812 — IC50 = 10000.0 nM 5.00
CHEMBL2170964 — IC50 > 2500.0 nM -
CHEMBL2170963 — IC50 - — -
CHEMBL2170960 — IC50 - — -
CHEMBL2170958 — IC50 - — -
CHEMBL2170817 — IC50 - — -