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Assay Detail

CHEMBL5541349

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Functional
Antiproliferative activity against human ICC13-7 cells assessed as inhibition of cell growth incubated for 3 days by Cell-titer glo assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type ICC13-7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
Tyhonas JS, Arnold LD, Cox JM, Franovic A, Gardiner E, Grandinetti K, Kania R, Kanouni T, Lardy M, Li C, Martin ES, Miller N, Mohan A, Murphy EA, Perez M, Soroceanu L, Timple N, Uryu S, Womble S, Kaldor SW.
J Med Chem (2024) 67 : 1734 -1746
PubMed 38267212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.66 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545376 ERDAFITINIB 4.0 1 8.96
CHEMBL5589734 1 8.85
CHEMBL3701238 FUTIBATINIB 4.0 1 8.74
CHEMBL5314537 RESIGRATINIB 2.0 1 8.70
CHEMBL5571671 1 8.66
CHEMBL4297522 PEMIGATINIB 4.0 1 8.59
CHEMBL1852688 INFIGRATINIB 4.0 1 8.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545376 ERDAFITINIB IC50 = 1.1 nM 8.96
CHEMBL5589734 IC50 = 1.4 nM 8.85
CHEMBL3701238 FUTIBATINIB IC50 = 1.8 nM 8.74
CHEMBL5314537 RESIGRATINIB IC50 = 2.0 nM 8.70
CHEMBL5571671 IC50 = 2.2 nM 8.66
CHEMBL4297522 PEMIGATINIB IC50 = 2.6 nM 8.59
CHEMBL1852688 INFIGRATINIB IC50 = 7.6 nM 8.12