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Assay Detail

CHEMBL862851

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

Binding
Inhibition of FGFR1
22
Total Activities
22
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 and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.
McBride CM, Renhowe PA, Heise C, Jansen JM, Lapointe G, Ma S, Piñeda R, Vora J, Wiesmann M, Shafer CM.
Bioorg Med Chem Lett (2006) 16 : 3595 -3599
PubMed 16603352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.37 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378024 1 9.00
CHEMBL377230 1 8.70
CHEMBL379740 1 8.52
CHEMBL377346 1 8.10
CHEMBL211662 1 7.82
CHEMBL379108 1 7.80
CHEMBL212429 1 7.75
CHEMBL209704 1 7.64
CHEMBL212054 1 7.55
CHEMBL378299 1 7.32
CHEMBL380372 1 7.14
CHEMBL208600 1 7.09
CHEMBL425247 1 7.03
CHEMBL208775 1 7.01
CHEMBL209783 1 7.00
CHEMBL211940 1 6.70
CHEMBL378003 1 6.68
CHEMBL209265 1 6.57
CHEMBL211708 1 6.08
CHEMBL383990 1 5.85
CHEMBL379995 1 -
CHEMBL212262 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378024 IC50 = 1.0 nM 9.00
CHEMBL377230 IC50 = 2.0 nM 8.70
CHEMBL379740 IC50 = 3.0 nM 8.52
CHEMBL377346 IC50 = 8.0 nM 8.10
CHEMBL211662 IC50 = 15.0 nM 7.82
CHEMBL379108 IC50 = 16.0 nM 7.80
CHEMBL212429 IC50 = 18.0 nM 7.75
CHEMBL209704 IC50 = 23.0 nM 7.64
CHEMBL212054 IC50 = 28.0 nM 7.55
CHEMBL378299 IC50 = 48.0 nM 7.32
CHEMBL380372 IC50 = 73.0 nM 7.14
CHEMBL208600 IC50 = 82.0 nM 7.09
CHEMBL425247 IC50 = 94.0 nM 7.03
CHEMBL208775 IC50 = 98.0 nM 7.01
CHEMBL209783 IC50 = 100.0 nM 7.00
CHEMBL211940 IC50 = 200.0 nM 6.70
CHEMBL378003 IC50 = 210.0 nM 6.68
CHEMBL209265 IC50 = 270.0 nM 6.57
CHEMBL211708 IC50 = 830.0 nM 6.08
CHEMBL383990 IC50 = 1400.0 nM 5.85
CHEMBL379995 IC50 > 3000.0 nM -
CHEMBL212262 IC50 > 3000.0 nM -