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Assay Detail

CHEMBL2027406

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

Binding
Inhibition of KDR
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.
Plé PA, Jung F, Ashton S, Hennequin L, Laine R, Lambert-van der Brempt C, Morgentin R, Pasquet G, Taylor S.
Bioorg Med Chem Lett (2012) 22 : 3050 -3055
PubMed 22497760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.42 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023485 1 8.52
CHEMBL2023486 1 8.40
CHEMBL1940274 1 8.10
CHEMBL2023476 1 7.70
CHEMBL2023482 1 7.70
CHEMBL2023494 1 7.64
CHEMBL2023118 1 7.17
CHEMBL2023117 1 7.09
CHEMBL2023490 1 6.74
CHEMBL2023800 1 6.61
CHEMBL1940275 1 6.31
CHEMBL2023483 1 6.29
CHEMBL2023484 1 5.89
CHEMBL2023478 1 5.79
CHEMBL2023477 1 5.72
CHEMBL2023119 1 5.68
CHEMBL2023492 1 5.61
CHEMBL2023488 1 5.40
CHEMBL2023475 1 5.39
CHEMBL2023474 1 5.37
CHEMBL2023495 1 5.33
CHEMBL2023116 1 5.32
CHEMBL2023802 1 5.32
CHEMBL2023489 1 4.96
CHEMBL2023115 1 -
CHEMBL2023479 1 -
CHEMBL2023480 1 -
CHEMBL2023481 1 -
CHEMBL2023487 1 -
CHEMBL2023491 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023485 IC50 = 3.0 nM 8.52
CHEMBL2023486 IC50 = 4.0 nM 8.40
CHEMBL1940274 IC50 = 8.0 nM 8.10
CHEMBL2023476 IC50 = 20.0 nM 7.70
CHEMBL2023482 IC50 = 20.0 nM 7.70
CHEMBL2023494 IC50 = 23.0 nM 7.64
CHEMBL2023118 IC50 = 67.0 nM 7.17
CHEMBL2023117 IC50 = 82.0 nM 7.09
CHEMBL2023490 IC50 = 183.0 nM 6.74
CHEMBL2023800 IC50 = 245.0 nM 6.61
CHEMBL1940275 IC50 = 485.0 nM 6.31
CHEMBL2023483 IC50 = 515.0 nM 6.29
CHEMBL2023484 IC50 = 1277.0 nM 5.89
CHEMBL2023478 IC50 = 1624.0 nM 5.79
CHEMBL2023477 IC50 = 1919.0 nM 5.72
CHEMBL2023119 IC50 = 2073.0 nM 5.68
CHEMBL2023492 IC50 = 2481.0 nM 5.61
CHEMBL2023488 IC50 = 3954.0 nM 5.40
CHEMBL2023475 IC50 = 4066.0 nM 5.39
CHEMBL2023474 IC50 = 4282.0 nM 5.37
CHEMBL2023495 IC50 = 4718.0 nM 5.33
CHEMBL2023116 IC50 = 4773.0 nM 5.32
CHEMBL2023802 IC50 = 4819.0 nM 5.32
CHEMBL2023489 IC50 = 10990.0 nM 4.96
CHEMBL2023115 IC50 > 690.0 nM -
CHEMBL2023479 IC50 > 10000.0 nM -
CHEMBL2023480 IC50 > 10000.0 nM -
CHEMBL2023481 IC50 > 10000.0 nM -
CHEMBL2023487 IC50 > 10000.0 nM -
CHEMBL2023491 IC50 > 10000.0 nM -
CHEMBL2023496 IC50 > 10000.0 nM -
CHEMBL2023801 IC50 > 8690.0 nM -
CHEMBL2023493 IC50 > 9740.0 nM -