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Assay Detail

CHEMBL1011001

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

Binding
Inhibition of human recombinant PDGFRbeta
40
Total Activities
40
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

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M, Lapointe GR, Feucht PH, Warne RL, Heise CC, Menezes D, Aardalen K, Ye H, He M, Le V, Vora J, Jansen JM, Wernette-Hammond ME, Harris AL.
J Med Chem (2009) 52 : 278 -292
PubMed 19113866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.28 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526507 1 10.00
CHEMBL495749 1 10.00
CHEMBL495984 1 9.70
CHEMBL495762 1 9.52
CHEMBL498551 1 9.52
CHEMBL498013 1 9.40
CHEMBL495735 1 9.22
CHEMBL495763 1 9.15
CHEMBL526285 1 9.05
CHEMBL498214 1 9.05
CHEMBL495962 1 9.00
CHEMBL496763 1 9.00
CHEMBL204427 1 8.70
CHEMBL495961 1 8.70
CHEMBL496762 1 8.70
CHEMBL522732 1 8.52
CHEMBL496150 1 8.40
CHEMBL498347 1 8.30
CHEMBL522892 DOVITINIB 3.0 1 8.30
CHEMBL523071 1 8.30
CHEMBL204426 1 8.30
CHEMBL526658 1 8.30
CHEMBL496764 1 8.15
CHEMBL495529 1 8.15
CHEMBL523745 1 8.10
CHEMBL449593 1 8.05
CHEMBL383417 1 8.00
CHEMBL498206 1 7.92
CHEMBL526836 1 7.85
CHEMBL377345 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526507 IC50 = 0.1 nM 10.00
CHEMBL495749 IC50 = 0.1 nM 10.00
CHEMBL495984 IC50 = 0.2 nM 9.70
CHEMBL495762 IC50 = 0.3 nM 9.52
CHEMBL498551 IC50 = 0.3 nM 9.52
CHEMBL498013 IC50 = 0.4 nM 9.40
CHEMBL495735 IC50 = 0.6 nM 9.22
CHEMBL495763 IC50 = 0.7 nM 9.15
CHEMBL526285 IC50 = 0.9 nM 9.05
CHEMBL498214 IC50 = 0.9 nM 9.05
CHEMBL495962 IC50 = 1.0 nM 9.00
CHEMBL496763 IC50 = 1.0 nM 9.00
CHEMBL204427 IC50 = 2.0 nM 8.70
CHEMBL495961 IC50 = 2.0 nM 8.70
CHEMBL496762 IC50 = 2.0 nM 8.70
CHEMBL522732 IC50 = 3.0 nM 8.52
CHEMBL496150 IC50 = 4.0 nM 8.40
CHEMBL526658 IC50 = 5.0 nM 8.30
CHEMBL204426 IC50 = 5.0 nM 8.30
CHEMBL522892 DOVITINIB IC50 = 5.0 nM 8.30
CHEMBL498347 IC50 = 5.0 nM 8.30
CHEMBL523071 IC50 = 5.0 nM 8.30
CHEMBL496764 IC50 = 7.0 nM 8.15
CHEMBL495529 IC50 = 7.0 nM 8.15
CHEMBL523745 IC50 = 8.0 nM 8.10
CHEMBL449593 IC50 = 9.0 nM 8.05
CHEMBL383417 IC50 = 10.0 nM 8.00
CHEMBL498206 IC50 = 12.0 nM 7.92
CHEMBL526836 IC50 = 14.0 nM 7.85
CHEMBL377345 IC50 = 20.0 nM 7.70
CHEMBL521552 IC50 = 30.0 nM 7.52
CHEMBL498205 IC50 = 30.0 nM 7.52
CHEMBL498348 IC50 = 30.0 nM 7.52
CHEMBL495530 IC50 = 39.0 nM 7.41
CHEMBL118440 IC50 = 70.0 nM 7.16
CHEMBL495983 IC50 = 70.0 nM 7.16
CHEMBL457985 IC50 = 130.0 nM 6.89
CHEMBL496172 IC50 = 1100.0 nM 5.96
CHEMBL523571 IC50 = 19000.0 nM 4.72
CHEMBL496173 IC50 > 25000.0 nM -