Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5583178

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

Functional
Inhibition of cell viability in human RT112/84 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RT112/84
Confidence 1 — Organism
Curated By Autocuration

Target

RT112/84 (CHEMBL6066783)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
Hudkins RL, Allen E, Balcer A, Hoffman ID, Iyer S, Neal M, Nelson KJ, Rideout M, Ye Q, Starrett JH, Patel P, Harris T, Swanson RV, Bensen DC.
J Med Chem (2024) 67 : 16737 -16756
PubMed 39258897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.91 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545376 ERDAFITINIB 4.0 1 8.44
CHEMBL5595947 1 8.08
CHEMBL5595500 1 8.05
CHEMBL5593800 1 8.04
CHEMBL5592211 1 7.89
CHEMBL5590817 1 7.82
CHEMBL5584069 1 7.57
CHEMBL5592556 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545376 ERDAFITINIB IC50 = 3.6 nM 8.44
CHEMBL5595947 IC50 = 8.3 nM 8.08
CHEMBL5595500 IC50 = 9.0 nM 8.05
CHEMBL5593800 IC50 = 9.2 nM 8.04
CHEMBL5592211 IC50 = 13.0 nM 7.89
CHEMBL5590817 IC50 = 15.0 nM 7.82
CHEMBL5584069 IC50 = 27.0 nM 7.57
CHEMBL5592556 IC50 = 38.0 nM 7.42