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Assay Detail

CHEMBL5100327

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

Binding
Inhibition of TEL-FGFR3 in mouse BaF3 cells incubated for 125 mins by plate reader analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 3 (CHEMBL4066)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Shvartsbart A, Roach JJ, Witten MR, Koblish H, Harris JJ, Covington M, Hess R, Lin L, Frascella M, Truong L, Leffet L, Conlen P, Beshad E, Klabe R, Katiyar K, Kaldon L, Young-Sciame R, He X, Petusky S, Chen KJ, Horsey A, Lei HT, Epling LB, Deller MC, Vechorkin O, Yao W.
J Med Chem (2022) 65 : 15433 -15442
PubMed 36356320 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.64 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187371 1 8.27
CHEMBL5180631 1 8.26
CHEMBL5203027 1 8.14
CHEMBL5206837 1 7.92
CHEMBL5184953 1 7.89
CHEMBL5202408 1 7.85
CHEMBL5200643 1 7.82
CHEMBL5172121 1 7.66
CHEMBL5202943 1 7.54
CHEMBL5199231 1 7.54
CHEMBL5201556 1 7.48
CHEMBL5196280 1 7.38
CHEMBL5174279 1 7.17
CHEMBL5208443 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187371 IC50 = 5.4 nM 8.27
CHEMBL5180631 IC50 = 5.5 nM 8.26
CHEMBL5203027 IC50 = 7.2 nM 8.14
CHEMBL5206837 IC50 = 12.0 nM 7.92
CHEMBL5184953 IC50 = 13.0 nM 7.89
CHEMBL5202408 IC50 = 14.0 nM 7.85
CHEMBL5200643 IC50 = 15.0 nM 7.82
CHEMBL5172121 IC50 = 22.0 nM 7.66
CHEMBL5202943 IC50 = 29.0 nM 7.54
CHEMBL5199231 IC50 = 29.0 nM 7.54
CHEMBL5201556 IC50 = 33.0 nM 7.48
CHEMBL5196280 IC50 = 42.0 nM 7.38
CHEMBL5174279 IC50 = 68.0 nM 7.17
CHEMBL5208443 IC50 = 969.0 nM 6.01