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Assay Detail

CHEMBL928636

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

Binding
Inhibition of human recombinant c-Met expressed in insect cell-baculovirus expression system
ChEMBL ↗
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.
Schroeder GM, Chen XT, Williams DK, Nirschl DS, Cai ZW, Wei D, Tokarski JS, An Y, Sack J, Chen Z, Huynh T, Vaccaro W, Poss M, Wautlet B, Gullo-Brown J, Kellar K, Manne V, Hunt JT, Wong TW, Lombardo LJ, Fargnoli J, Borzilleri RM.
Bioorg Med Chem Lett (2008) 18 : 1945 -1951
PubMed 18289854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.85 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254086 — — 1 8.82
CHEMBL255092 — — 1 7.52
CHEMBL400332 — — 1 7.52
CHEMBL254280 — — 1 7.52
CHEMBL254085 — — 1 7.43
CHEMBL255091 — — 1 7.40
CHEMBL399698 — — 1 7.40
CHEMBL438696 — — 1 7.40
CHEMBL253881 — — 1 7.35
CHEMBL413996 — — 1 7.30
CHEMBL251782 — — 1 7.16
CHEMBL253222 — — 1 7.16
CHEMBL254879 — — 1 7.05
CHEMBL399920 — — 1 7.05
CHEMBL251780 — — 1 7.05
CHEMBL401344 — — 1 6.89
CHEMBL254907 — — 1 6.85
CHEMBL429490 — — 1 6.82
CHEMBL400556 — — 1 6.82
CHEMBL251980 — — 1 6.80
CHEMBL400726 — — 1 6.75
CHEMBL428944 — — 1 6.72
CHEMBL399674 — — 1 6.72
CHEMBL252213 — — 1 6.58
CHEMBL252415 — — 1 6.39
CHEMBL253444 — — 1 6.36
CHEMBL253657 — — 1 6.36
CHEMBL430026 — — 1 6.29
CHEMBL399710 — — 1 6.12
CHEMBL253223 — — 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254086 — IC50 = 1.5 nM 8.82
CHEMBL255092 — IC50 = 30.0 nM 7.52
CHEMBL254280 — IC50 = 30.0 nM 7.52
CHEMBL400332 — IC50 = 30.0 nM 7.52
CHEMBL254085 — IC50 = 37.0 nM 7.43
CHEMBL255091 — IC50 = 40.0 nM 7.40
CHEMBL399698 — IC50 = 40.0 nM 7.40
CHEMBL438696 — IC50 = 40.0 nM 7.40
CHEMBL253881 — IC50 = 45.0 nM 7.35
CHEMBL413996 — IC50 = 50.0 nM 7.30
CHEMBL251782 — IC50 = 70.0 nM 7.16
CHEMBL253222 — IC50 = 70.0 nM 7.16
CHEMBL254879 — IC50 = 90.0 nM 7.05
CHEMBL399920 — IC50 = 90.0 nM 7.05
CHEMBL251780 — IC50 = 90.0 nM 7.05
CHEMBL401344 — IC50 = 130.0 nM 6.89
CHEMBL254907 — IC50 = 140.0 nM 6.85
CHEMBL400556 — IC50 = 150.0 nM 6.82
CHEMBL429490 — IC50 = 150.0 nM 6.82
CHEMBL251980 — IC50 = 160.0 nM 6.80
CHEMBL400726 — IC50 = 180.0 nM 6.75
CHEMBL428944 — IC50 = 190.0 nM 6.72
CHEMBL399674 — IC50 = 190.0 nM 6.72
CHEMBL252213 — IC50 = 260.0 nM 6.58
CHEMBL252415 — IC50 = 410.0 nM 6.39
CHEMBL253444 — IC50 = 440.0 nM 6.36
CHEMBL253657 — IC50 = 440.0 nM 6.36
CHEMBL430026 — IC50 = 510.0 nM 6.29
CHEMBL399710 — IC50 = 760.0 nM 6.12
CHEMBL253223 — IC50 = 780.0 nM 6.11
CHEMBL252416 — IC50 = 860.0 nM 6.07
CHEMBL253882 — IC50 = 900.0 nM 6.05
CHEMBL253656 — IC50 = 990.0 nM 6.00
CHEMBL430027 — IC50 = 1000.0 nM 6.00
CHEMBL252214 — IC50 = 1400.0 nM 5.85
CHEMBL254281 — IC50 > 2000.0 nM -