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Assay Detail

CHEMBL833382

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Functional
Concentration required to inhibit proliferation of HUVEC
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HUVEC
Confidence 1 — Organism
Curated By Intermediate

Target

HUVEC (CHEMBL613979)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.
J Med Chem (2005) 48 : 4892 -4909
PubMed 16033269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.90 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190984 1 6.06
CHEMBL372657 1 5.97
CHEMBL188386 1 5.93
CHEMBL371169 1 5.86
CHEMBL177688 1 5.78
CHEMBL188502 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190984 IC50 = 877.0 nM 6.06
CHEMBL372657 IC50 = 1070.0 nM 5.97
CHEMBL188386 IC50 = 1170.0 nM 5.93
CHEMBL371169 IC50 = 1390.0 nM 5.86
CHEMBL177688 IC50 = 1680.0 nM 5.78
CHEMBL188502 IC50 = 1670.0 nM 5.78