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Assay Detail

CHEMBL4715301

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 as substrate preincubated for 10 mins followed by ATP addition by phosphoenolpyruvate/pyruvate kinase/lactate dehydrogenase coupled radiometric assay
21
Total Activities
21
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

Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Tang Q,Aronov AM,Deininger DD,Giroux S,Lauffer DJ,Li P,Liang J,McGinty K,Ronkin S,Swett R,Waal N,Boucher D,Ford PJ,Moody CS
ACS Med Chem Lett (2021) 12 : 955 -960
PubMed 34141080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.33 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784332 1 8.15
CHEMBL4753090 1 8.10
CHEMBL4790331 1 8.00
CHEMBL4783289 1 7.82
CHEMBL4787386 1 7.70
CHEMBL4791034 1 7.70
CHEMBL4778083 1 7.68
CHEMBL4750387 1 7.62
CHEMBL4793526 1 7.52
CHEMBL4786582 1 7.40
CHEMBL4760101 1 7.40
CHEMBL4743756 1 7.30
CHEMBL4762193 1 7.30
CHEMBL2170957 1 7.22
CHEMBL4740644 1 7.10
CHEMBL4748465 1 7.10
CHEMBL4740776 1 6.70
CHEMBL2431818 1 6.70
CHEMBL4763399 1 6.62
CHEMBL4764695 1 6.40
CHEMBL1822377 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784332 Ki = 7.0 nM 8.15
CHEMBL4753090 Ki = 8.0 nM 8.10
CHEMBL4790331 Ki = 10.0 nM 8.00
CHEMBL4783289 Ki = 15.0 nM 7.82
CHEMBL4787386 Ki = 20.0 nM 7.70
CHEMBL4791034 Ki = 20.0 nM 7.70
CHEMBL4778083 Ki = 21.0 nM 7.68
CHEMBL4750387 Ki = 24.0 nM 7.62
CHEMBL4793526 Ki = 30.0 nM 7.52
CHEMBL4786582 Ki = 40.0 nM 7.40
CHEMBL4760101 Ki = 40.0 nM 7.40
CHEMBL4743756 Ki = 50.0 nM 7.30
CHEMBL4762193 Ki = 50.0 nM 7.30
CHEMBL2170957 Ki = 60.0 nM 7.22
CHEMBL4740644 Ki = 80.0 nM 7.10
CHEMBL4748465 Ki = 80.0 nM 7.10
CHEMBL4740776 Ki = 200.0 nM 6.70
CHEMBL2431818 Ki = 200.0 nM 6.70
CHEMBL4763399 Ki = 240.0 nM 6.62
CHEMBL4764695 Ki = 400.0 nM 6.40
CHEMBL1822377 Ki = 400.0 nM 6.40