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Assay Detail

CHEMBL5583156

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

Binding
Inhibition of recombinant BCR/FGFR1 (unknown origin) transduced in mouse BaF3 cells incubated for 48 hrs by Cell Titer Glo assay
ChEMBL ↗
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

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 44 6.73 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828009 LY-2874455 1.0 1 9.30
CHEMBL3545376 ERDAFITINIB 4.0 1 8.28
CHEMBL5594526 — — 1 7.85
CHEMBL5589661 — — 1 7.34
CHEMBL5595860 — — 1 7.23
CHEMBL5592858 — — 1 7.22
CHEMBL5593614 — — 1 7.21
CHEMBL5595265 — — 1 7.08
CHEMBL5595732 — — 1 7.03
CHEMBL5590027 — — 1 7.00
CHEMBL5593800 — — 1 6.98
CHEMBL5593851 — — 1 6.95
CHEMBL5591378 — — 1 6.95
CHEMBL5595947 — — 1 6.89
CHEMBL5594411 — — 1 6.87
CHEMBL5591286 — — 1 6.82
CHEMBL5595996 — — 1 6.76
CHEMBL5593595 — — 1 6.75
CHEMBL5592556 — — 1 6.75
CHEMBL5593620 — — 1 6.72
CHEMBL5584069 — — 1 6.69
CHEMBL5592315 — — 1 6.68
CHEMBL5590817 — — 1 6.67
CHEMBL5594474 — — 1 6.64
CHEMBL5594121 — — 1 6.63
CHEMBL5594093 — — 1 6.59
CHEMBL5595500 — — 1 6.56
CHEMBL5594702 — — 1 6.54
CHEMBL5594646 — — 1 6.54
CHEMBL5595795 — — 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828009 LY-2874455 IC50 = 0.5 nM 9.30
CHEMBL3545376 ERDAFITINIB IC50 = 5.2 nM 8.28
CHEMBL5594526 — IC50 = 14.0 nM 7.85
CHEMBL5589661 — IC50 = 46.0 nM 7.34
CHEMBL5595860 — IC50 = 59.0 nM 7.23
CHEMBL5592858 — IC50 = 60.0 nM 7.22
CHEMBL5593614 — IC50 = 61.0 nM 7.21
CHEMBL5595265 — IC50 = 84.0 nM 7.08
CHEMBL5595732 — IC50 = 94.0 nM 7.03
CHEMBL5590027 — IC50 = 99.0 nM 7.00
CHEMBL5593800 — IC50 = 104.0 nM 6.98
CHEMBL5591378 — IC50 = 112.0 nM 6.95
CHEMBL5593851 — IC50 = 113.0 nM 6.95
CHEMBL5595947 — IC50 = 129.0 nM 6.89
CHEMBL5594411 — IC50 = 135.0 nM 6.87
CHEMBL5591286 — IC50 = 150.0 nM 6.82
CHEMBL5595996 — IC50 = 172.0 nM 6.76
CHEMBL5593595 — IC50 = 176.0 nM 6.75
CHEMBL5592556 — IC50 = 179.0 nM 6.75
CHEMBL5593620 — IC50 = 189.0 nM 6.72
CHEMBL5584069 — IC50 = 204.0 nM 6.69
CHEMBL5592315 — IC50 = 208.0 nM 6.68
CHEMBL5590817 — IC50 = 212.0 nM 6.67
CHEMBL5594474 — IC50 = 228.0 nM 6.64
CHEMBL5594121 — IC50 = 234.0 nM 6.63
CHEMBL5594093 — IC50 = 258.0 nM 6.59
CHEMBL5595500 — IC50 = 278.0 nM 6.56
CHEMBL5594702 — IC50 = 290.0 nM 6.54
CHEMBL5594646 — IC50 = 290.0 nM 6.54
CHEMBL5595795 — IC50 = 338.0 nM 6.47
CHEMBL5595523 — IC50 = 390.0 nM 6.41
CHEMBL5592211 — IC50 = 401.0 nM 6.40
CHEMBL5594268 — IC50 = 405.0 nM 6.39
CHEMBL5595644 — IC50 = 423.0 nM 6.37
CHEMBL5583622 — IC50 = 434.0 nM 6.36
CHEMBL5594969 — IC50 = 514.0 nM 6.29
CHEMBL5590821 — IC50 = 556.0 nM 6.25
CHEMBL5594925 — IC50 = 653.0 nM 6.18
CHEMBL5584096 — IC50 = 711.0 nM 6.15
CHEMBL5592520 — IC50 = 872.0 nM 6.06
CHEMBL5594509 — IC50 = 880.0 nM 6.06
CHEMBL5594374 — IC50 = 1043.0 nM 5.98
CHEMBL5593361 — IC50 = 2003.0 nM 5.70
CHEMBL5593408 — IC50 = 2198.0 nM 5.66