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Assay Detail

CHEMBL825076

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

Functional
Inhibition of FGF-stimulated human umbilical vein endothelial cell proliferation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Endothelial cell
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Fibroblast growth factor receptor (CHEMBL2095217)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.
J Med Chem (2005) 48 : 3991 -4008
PubMed 15943473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373365 1 9.00
CHEMBL193306 1 8.40
CHEMBL195398 1 8.34
CHEMBL371373 1 8.33
CHEMBL190980 1 8.28
CHEMBL365318 1 8.19
CHEMBL192101 1 8.18
CHEMBL195847 1 8.14
CHEMBL370515 1 8.12
CHEMBL191913 1 8.04
CHEMBL194498 1 7.68
CHEMBL370023 1 7.48
CHEMBL194872 1 7.36
CHEMBL193136 1 7.34
CHEMBL195771 1 7.27
CHEMBL195903 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373365 IC50 = 1.0 nM 9.00
CHEMBL193306 IC50 = 4.0 nM 8.40
CHEMBL195398 IC50 = 4.6 nM 8.34
CHEMBL371373 IC50 = 4.7 nM 8.33
CHEMBL190980 IC50 = 5.3 nM 8.28
CHEMBL365318 IC50 = 6.5 nM 8.19
CHEMBL192101 IC50 = 6.6 nM 8.18
CHEMBL195847 IC50 = 7.3 nM 8.14
CHEMBL370515 IC50 = 7.6 nM 8.12
CHEMBL191913 IC50 = 9.2 nM 8.04
CHEMBL194498 IC50 = 21.0 nM 7.68
CHEMBL370023 IC50 = 33.0 nM 7.48
CHEMBL194872 IC50 = 44.0 nM 7.36
CHEMBL193136 IC50 = 46.0 nM 7.34
CHEMBL195771 IC50 = 54.0 nM 7.27
CHEMBL195903 IC50 = 130.0 nM 6.89