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Assay Detail

CHEMBL3268019

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

Binding
Inhibition of c-Met (unknown origin) using poly Glu:Tyr (4:1) as substrate after 60 mins by ELISA
22
Total Activities
22
Compounds Tested
2
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

Discovery of novel type II c-Met inhibitors based on BMS-777607.
Zhang W, Ai J, Shi D, Peng X, Ji Y, Liu J, Geng M, Li Y.
Eur J Med Chem (2014) 80 : 254 -266
PubMed 24792774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.27 9.15
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3260966 1 9.15
CHEMBL3260967 1 9.05
CHEMBL3260968 1 8.77
CHEMBL460702 BMS-777607 2.0 1 8.43
CHEMBL3260962 1 7.70
CHEMBL3260964 1 7.57
CHEMBL3091589 1 7.41
CHEMBL3260965 1 7.30
CHEMBL3260953 1 7.15
CHEMBL3260961 1 7.09
CHEMBL3260954 1 7.00
CHEMBL3260952 1 6.78
CHEMBL3260951 1 6.77
CHEMBL3260948 1 6.54
CHEMBL3260950 1 6.43
CHEMBL3260960 1 6.37
CHEMBL3260956 1 6.36
CHEMBL3260949 1 6.31
CHEMBL3260955 1 5.98
CHEMBL3260959 1 -
CHEMBL3260958 1 -
CHEMBL3260957 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3260966 IC50 = 0.7 nM 9.15
CHEMBL3260967 IC50 = 0.9 nM 9.05
CHEMBL3260968 IC50 = 1.7 nM 8.77
CHEMBL460702 BMS-777607 IC50 = 3.7 nM 8.43
CHEMBL3260962 IC50 = 20.0 nM 7.70
CHEMBL3260964 IC50 = 26.9 nM 7.57
CHEMBL3091589 IC50 = 39.0 nM 7.41
CHEMBL3260965 IC50 = 49.6 nM 7.30
CHEMBL3260953 IC50 = 70.2 nM 7.15
CHEMBL3260961 IC50 = 81.0 nM 7.09
CHEMBL3260954 IC50 = 100.8 nM 7.00
CHEMBL3260952 IC50 = 165.5 nM 6.78
CHEMBL3260951 IC50 = 168.7 nM 6.77
CHEMBL3260948 IC50 = 290.5 nM 6.54
CHEMBL3260950 IC50 = 373.2 nM 6.43
CHEMBL3260960 IC50 = 427.0 nM 6.37
CHEMBL3260956 IC50 = 432.9 nM 6.36
CHEMBL3260949 IC50 = 494.7 nM 6.31
CHEMBL3260955 IC50 = 1044.0 nM 5.98
CHEMBL3260959 Inhibition - % -
CHEMBL3260958 IC50 - -
CHEMBL3260957 Inhibition - % -