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Assay Detail

CHEMBL895899

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

Functional
Inhibition of KDR phosphorylation
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors.
Potashman MH, Bready J, Coxon A, DeMelfi TM, DiPietro L, Doerr N, Elbaum D, Estrada J, Gallant P, Germain J, Gu Y, Harmange JC, Kaufman SA, Kendall R, Kim JL, Kumar GN, Long AM, Neervannan S, Patel VF, Polverino A, Rose P, Plas Sv, Whittington D, Zanon R, Zhao H.
J Med Chem (2007) 50 : 4351 -4373
PubMed 17696416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 8.27 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427837 1 9.70
CHEMBL230003 1 9.30
CHEMBL389963 1 9.30
CHEMBL230107 1 9.30
CHEMBL231370 1 9.00
CHEMBL230222 1 8.80
CHEMBL387591 1 8.70
CHEMBL397496 1 8.70
CHEMBL231269 1 8.70
CHEMBL387590 1 8.70
CHEMBL231568 1 8.55
CHEMBL397497 1 8.52
CHEMBL231168 1 8.52
CHEMBL425672 1 8.52
CHEMBL230002 1 8.52
CHEMBL230223 1 8.52
CHEMBL390175 1 8.44
CHEMBL413621 1 8.41
CHEMBL231570 1 8.40
CHEMBL231569 1 8.40
CHEMBL231469 1 8.40
CHEMBL395335 1 8.30
CHEMBL396265 1 8.10
CHEMBL394826 1 8.05
CHEMBL231067 1 8.05
CHEMBL395334 1 8.00
CHEMBL425831 1 8.00
CHEMBL1162958 1 7.92
CHEMBL231371 1 7.77
CHEMBL425825 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427837 Ki = 0.2 nM 9.70
CHEMBL230003 Ki = 0.5 nM 9.30
CHEMBL389963 Ki = 0.5 nM 9.30
CHEMBL230107 Ki = 0.5 nM 9.30
CHEMBL231370 Ki = 1.0 nM 9.00
CHEMBL230222 Ki = 1.6 nM 8.80
CHEMBL387591 Ki = 2.0 nM 8.70
CHEMBL397496 Ki = 2.0 nM 8.70
CHEMBL231269 Ki = 2.0 nM 8.70
CHEMBL387590 Ki = 2.0 nM 8.70
CHEMBL231568 Ki = 2.8 nM 8.55
CHEMBL230002 Ki = 3.0 nM 8.52
CHEMBL425672 Ki = 3.0 nM 8.52
CHEMBL230223 Ki = 3.0 nM 8.52
CHEMBL231168 Ki = 3.0 nM 8.52
CHEMBL397497 Ki = 3.0 nM 8.52
CHEMBL390175 Ki = 3.6 nM 8.44
CHEMBL413621 Ki = 3.9 nM 8.41
CHEMBL231570 Ki = 4.0 nM 8.40
CHEMBL231469 Ki = 4.0 nM 8.40
CHEMBL231569 Ki = 4.0 nM 8.40
CHEMBL395335 Ki = 5.0 nM 8.30
CHEMBL396265 Ki = 8.0 nM 8.10
CHEMBL394826 Ki = 9.0 nM 8.05
CHEMBL231067 Ki = 9.0 nM 8.05
CHEMBL395334 Ki = 10.0 nM 8.00
CHEMBL425831 Ki = 10.0 nM 8.00
CHEMBL1162958 Ki = 12.0 nM 7.92
CHEMBL231371 Ki = 17.0 nM 7.77
CHEMBL425825 Ki = 20.0 nM 7.70
CHEMBL230109 Ki = 25.0 nM 7.60
CHEMBL231467 Ki = 40.0 nM 7.40
CHEMBL427264 Ki = 48.0 nM 7.32
CHEMBL231468 Ki = 128.0 nM 6.89
CHEMBL231066 Ki = 160.0 nM 6.80
CHEMBL231270 Ki = 287.0 nM 6.54