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Assay Detail

CHEMBL1837640

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

Functional
Antiproliferative activity against mouse BAF3 cell line transformed with TEL-FGFR3 construct after 48 hrs by luciferase bioluminescent assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H, Wartmann M, Berghausen J, Drueckes P, Zimmerlin A, Bussiere D, Murray J, Graus Porta D.
J Med Chem (2011) 54 : 7066 -7083
PubMed 21936542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.13 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1834658 1 8.70
CHEMBL1834657 INFIGRATINIB PHOSPHATE 4.0 1 8.70
CHEMBL1834663 1 7.96
CHEMBL1834662 1 7.85
CHEMBL1834661 1 7.85
CHEMBL1834660 1 7.57
CHEMBL1834659 1 7.55
CHEMBL1834656 1 6.93
CHEMBL1834655 1 6.90
CHEMBL1834603 1 6.20
CHEMBL1833981 1 6.12
CHEMBL1834653 1 6.08
CHEMBL1834602 1 5.82
CHEMBL1834654 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1834658 IC50 = 2.0 nM 8.70
CHEMBL1834657 INFIGRATINIB PHOSPHATE IC50 = 2.0 nM 8.70
CHEMBL1834663 IC50 = 11.0 nM 7.96
CHEMBL1834662 IC50 = 14.0 nM 7.85
CHEMBL1834661 IC50 = 14.0 nM 7.85
CHEMBL1834660 IC50 = 27.0 nM 7.57
CHEMBL1834659 IC50 = 28.0 nM 7.55
CHEMBL1834656 IC50 = 118.0 nM 6.93
CHEMBL1834655 IC50 = 126.0 nM 6.90
CHEMBL1834603 IC50 = 635.0 nM 6.20
CHEMBL1833981 IC50 = 750.0 nM 6.12
CHEMBL1834653 IC50 = 832.0 nM 6.08
CHEMBL1834602 IC50 = 1512.0 nM 5.82
CHEMBL1834654 IC50 = 2223.0 nM 5.65