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Assay Detail

CHEMBL829448

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

Binding
Inhibition of human fibroblast growth factor receptor 1
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fibroblast growth factor receptor 1 (CHEMBL3650)
Type SINGLE PROTEIN
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 19 7.32 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190980 1 7.85
CHEMBL195398 1 7.80
CHEMBL195847 1 7.75
CHEMBL365318 1 7.72
CHEMBL193306 1 7.70
CHEMBL191913 1 7.57
CHEMBL371373 1 7.55
CHEMBL192101 1 7.48
CHEMBL373365 1 7.41
CHEMBL370266 1 7.34
CHEMBL193136 1 7.30
CHEMBL195218 1 7.24
CHEMBL194872 1 7.17
CHEMBL370023 1 7.08
CHEMBL370515 1 6.96
CHEMBL194929 1 6.85
CHEMBL372662 1 6.83
CHEMBL195771 1 6.80
CHEMBL195903 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190980 IC50 = 14.0 nM 7.85
CHEMBL195398 IC50 = 16.0 nM 7.80
CHEMBL195847 IC50 = 18.0 nM 7.75
CHEMBL365318 IC50 = 19.0 nM 7.72
CHEMBL193306 IC50 = 20.0 nM 7.70
CHEMBL191913 IC50 = 27.0 nM 7.57
CHEMBL371373 IC50 = 28.0 nM 7.55
CHEMBL192101 IC50 = 33.0 nM 7.48
CHEMBL373365 IC50 = 39.0 nM 7.41
CHEMBL370266 IC50 = 46.0 nM 7.34
CHEMBL193136 IC50 = 50.0 nM 7.30
CHEMBL195218 IC50 = 58.0 nM 7.24
CHEMBL194872 IC50 = 68.0 nM 7.17
CHEMBL370023 IC50 = 84.0 nM 7.08
CHEMBL370515 IC50 = 110.0 nM 6.96
CHEMBL194929 IC50 = 140.0 nM 6.85
CHEMBL372662 IC50 = 149.0 nM 6.83
CHEMBL195771 IC50 = 160.0 nM 6.80
CHEMBL195903 IC50 = 220.0 nM 6.66