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Assay Detail

CHEMBL832771

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

Binding
Inhibition of platelet-derived growth factor receptor alpha
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Platelet-derived growth factor receptor alpha (CHEMBL2007)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.
Kubo K, Shimizu T, Ohyama S, Murooka H, Iwai A, Nakamura K, Hasegawa K, Kobayashi Y, Takahashi N, Takahashi K, Kato S, Izawa T, Isoe T.
J Med Chem (2005) 48 : 1359 -1366
PubMed 15743179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.97 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179698 1 8.80
CHEMBL179593 1 8.70
CHEMBL178156 1 8.70
CHEMBL369760 1 8.48
CHEMBL360526 1 8.47
CHEMBL179307 1 8.46
CHEMBL179603 1 8.44
CHEMBL368252 1 8.44
CHEMBL179061 1 8.44
CHEMBL179227 1 8.41
CHEMBL179522 1 8.33
CHEMBL426047 1 8.24
CHEMBL180331 1 8.24
CHEMBL426602 1 8.19
CHEMBL360781 1 8.17
CHEMBL179719 1 8.17
CHEMBL179816 1 8.00
CHEMBL179165 1 8.00
CHEMBL362486 1 7.85
CHEMBL178568 1 7.77
CHEMBL179360 1 7.75
CHEMBL179753 1 7.68
CHEMBL362188 1 7.62
CHEMBL178981 1 7.62
CHEMBL362634 1 7.44
CHEMBL179422 1 7.43
CHEMBL369747 1 7.37
CHEMBL178276 1 7.28
CHEMBL359617 1 7.26
CHEMBL440202 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179698 IC50 = 1.6 nM 8.80
CHEMBL179593 IC50 = 2.0 nM 8.70
CHEMBL178156 IC50 = 2.0 nM 8.70
CHEMBL369760 IC50 = 3.3 nM 8.48
CHEMBL360526 IC50 = 3.4 nM 8.47
CHEMBL179307 IC50 = 3.5 nM 8.46
CHEMBL179603 IC50 = 3.6 nM 8.44
CHEMBL368252 IC50 = 3.6 nM 8.44
CHEMBL179061 IC50 = 3.6 nM 8.44
CHEMBL179227 IC50 = 3.9 nM 8.41
CHEMBL179522 IC50 = 4.7 nM 8.33
CHEMBL426047 IC50 = 5.8 nM 8.24
CHEMBL180331 IC50 = 5.8 nM 8.24
CHEMBL426602 IC50 = 6.4 nM 8.19
CHEMBL179719 IC50 = 6.8 nM 8.17
CHEMBL360781 IC50 = 6.8 nM 8.17
CHEMBL179816 IC50 = 10.0 nM 8.00
CHEMBL179165 IC50 = 10.0 nM 8.00
CHEMBL362486 IC50 = 14.0 nM 7.85
CHEMBL178568 IC50 = 17.0 nM 7.77
CHEMBL179360 IC50 = 18.0 nM 7.75
CHEMBL179753 IC50 = 21.0 nM 7.68
CHEMBL362188 IC50 = 24.0 nM 7.62
CHEMBL178981 IC50 = 24.0 nM 7.62
CHEMBL362634 IC50 = 36.0 nM 7.44
CHEMBL179422 IC50 = 37.0 nM 7.43
CHEMBL369747 IC50 = 43.0 nM 7.37
CHEMBL178276 IC50 = 52.0 nM 7.28
CHEMBL359617 IC50 = 55.0 nM 7.26
CHEMBL440202 IC50 = 75.0 nM 7.12
CHEMBL179450 IC50 = 490.0 nM 6.31
CHEMBL179082 IC50 < 10.0 nM -