Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL770471

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

Functional
Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in rat aorta vascular smooth muscle cells.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Platelet-derived growth factor receptor (PDGFr) (CHEMBL2111344)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor.
Palmer BD, Smaill JB, Boyd M, Boschelli DH, Doherty AM, Hamby JM, Khatana SS, Kramer JB, Kraker AJ, Panek RL, Lu GH, Dahring TK, Winters RT, Showalter HD, Denny WA.
J Med Chem (1998) 41 : 5457 -5465
PubMed 9876115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.15 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80873 1 6.89
CHEMBL153054 1 6.82
CHEMBL76202 1 5.72
CHEMBL346870 1 5.70
CHEMBL310080 1 5.64
CHEMBL75964 1 -
CHEMBL356169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80873 IC50 = 130.0 nM 6.89
CHEMBL153054 IC50 = 150.0 nM 6.82
CHEMBL76202 IC50 = 1900.0 nM 5.72
CHEMBL346870 IC50 = 2000.0 nM 5.70
CHEMBL310080 IC50 = 2300.0 nM 5.64
CHEMBL75964 IC50 > 10000.0 nM -
CHEMBL356169 IC50 > 10000.0 nM -