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Assay Detail

CHEMBL969890

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Binding
Inhibition of human activated c-Met by PK/LDH coupled kinetic assay
16
Total Activities
16
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 activity relationships of quinoline-containing c-Met inhibitors.
Kung PP, Funk L, Meng J, Alton G, Padrique E, Mroczkowski B.
Eur J Med Chem (2008) 43 : 1321 -1329
PubMed 17964000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.53 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404881 1 9.00
CHEMBL205372 1 8.70
CHEMBL510112 1 8.52
CHEMBL472552 1 7.30
CHEMBL461998 1 7.10
CHEMBL518511 1 6.40
CHEMBL461120 1 6.30
CHEMBL461119 1 6.30
CHEMBL459892 1 6.00
CHEMBL461118 1 6.00
CHEMBL518357 1 5.55
CHEMBL460944 1 5.30
CHEMBL462171 1 5.19
CHEMBL462183 1 5.16
CHEMBL462357 1 5.10
CHEMBL462358 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404881 Ki = 1.0 nM 9.00
CHEMBL205372 Ki = 2.0 nM 8.70
CHEMBL510112 Ki = 3.0 nM 8.52
CHEMBL472552 Ki = 50.0 nM 7.30
CHEMBL461998 Ki = 80.0 nM 7.10
CHEMBL518511 Ki = 400.0 nM 6.40
CHEMBL461120 Ki = 500.0 nM 6.30
CHEMBL461119 Ki = 500.0 nM 6.30
CHEMBL459892 Ki = 1000.0 nM 6.00
CHEMBL461118 Ki = 1000.0 nM 6.00
CHEMBL518357 Ki = 2800.0 nM 5.55
CHEMBL460944 Ki = 5000.0 nM 5.30
CHEMBL462171 Ki = 6400.0 nM 5.19
CHEMBL462183 Ki = 7000.0 nM 5.16
CHEMBL462357 Ki = 8000.0 nM 5.10
CHEMBL462358 Ki > 30000.0 nM -