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

CHEMBL5583159

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

Binding
Inhibition of recombinant TEL/VEGFR2 (unknown origin) transduced in mouse BaF3 cells incubated for 48 hrs by Cell Titer Glo assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

TEL/KDR (CHEMBL4630759)
Type CHIMERIC PROTEIN
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 14 6.47 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828009 LY-2874455 1.0 1 8.05
CHEMBL5593851 1 6.79
CHEMBL5591286 1 6.70
CHEMBL5591378 1 6.50
CHEMBL5594702 1 6.49
CHEMBL5595996 1 6.25
CHEMBL5590027 1 6.23
CHEMBL3545376 ERDAFITINIB 4.0 1 6.20
CHEMBL5590821 1 6.20
CHEMBL5594925 1 6.17
CHEMBL5594374 1 6.06
CHEMBL5594969 1 6.05
CHEMBL5589661 1 -
CHEMBL5595795 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828009 LY-2874455 IC50 = 9.0 nM 8.05
CHEMBL5593851 IC50 = 162.0 nM 6.79
CHEMBL5591286 IC50 = 198.0 nM 6.70
CHEMBL5591378 IC50 = 314.0 nM 6.50
CHEMBL5594702 IC50 = 323.0 nM 6.49
CHEMBL5595996 IC50 = 560.0 nM 6.25
CHEMBL5590027 IC50 = 586.0 nM 6.23
CHEMBL3545376 ERDAFITINIB IC50 = 627.0 nM 6.20
CHEMBL5590821 IC50 = 637.0 nM 6.20
CHEMBL5594925 IC50 = 679.0 nM 6.17
CHEMBL5594374 IC50 = 864.0 nM 6.06
CHEMBL5594969 IC50 = 887.0 nM 6.05
CHEMBL5589661 IC50 - -
CHEMBL5595795 IC50 - -