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Assay Detail

CHEMBL5239772

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

Functional
Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Huh-7 (CHEMBL614039)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 2-Amino-7-sulfonyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.
Xie W, Yang S, Liang L, Wang M, Zuo W, Lei Y, Zhang Y, Tang W, Lu T, Chen Y, Jiang Y.
J Med Chem (2022) 65 : 16570 -16588
PubMed 36480917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.58 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4514636 FISOGATINIB 2.0 1 7.34
CHEMBL5278656 1 7.02
CHEMBL5281307 1 6.88
CHEMBL5289886 1 6.78
CHEMBL5283096 1 6.72
CHEMBL5280802 1 6.62
CHEMBL5290554 1 6.61
CHEMBL5268564 1 6.53
CHEMBL5283169 1 6.52
CHEMBL5268351 1 6.51
CHEMBL5280110 1 6.42
CHEMBL5290407 1 6.42
CHEMBL5283222 1 6.35
CHEMBL5267668 1 6.35
CHEMBL5279776 1 6.35
CHEMBL5275506 1 6.27
CHEMBL5272254 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4514636 FISOGATINIB IC50 = 45.9 nM 7.34
CHEMBL5278656 IC50 = 94.7 nM 7.02
CHEMBL5281307 IC50 = 131.4 nM 6.88
CHEMBL5289886 IC50 = 166.4 nM 6.78
CHEMBL5283096 IC50 = 191.1 nM 6.72
CHEMBL5280802 IC50 = 240.1 nM 6.62
CHEMBL5290554 IC50 = 244.5 nM 6.61
CHEMBL5268564 IC50 = 298.2 nM 6.53
CHEMBL5283169 IC50 = 301.0 nM 6.52
CHEMBL5268351 IC50 = 310.1 nM 6.51
CHEMBL5280110 IC50 = 382.9 nM 6.42
CHEMBL5290407 IC50 = 376.7 nM 6.42
CHEMBL5283222 IC50 = 449.0 nM 6.35
CHEMBL5267668 IC50 = 451.2 nM 6.35
CHEMBL5279776 IC50 = 443.7 nM 6.35
CHEMBL5275506 IC50 = 534.2 nM 6.27
CHEMBL5272254 IC50 = 811.4 nM 6.09