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Assay Detail

CHEMBL5240446

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Functional
Antiproliferative activity against human UM-UC-9 assessed as inhibition of cell proliferation measured after 7 days by IncuCyte live-cell imaging assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type UM-UC-9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Orsi DL, Ferrara SJ, Siegel S, Friberg A, Bouché L, Pook E, Lienau P, Bluck JP, Lemke CT, Akcay G, Stellfeld T, Meyer H, Pütter V, Holton SJ, Korr D, Jerchel-Furau I, Pantelidou C, Strathdee CA, Meyerson M, Eis K, Goldstein JT.
Bioorg Med Chem (2023) 78 : 117130 -117130
PubMed 36542958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.85 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5281842 1 7.73
CHEMBL5267263 1 7.71
CHEMBL5282503 1 7.51
CHEMBL5286386 1 7.39
CHEMBL5272194 1 7.20
CHEMBL5273393 1 7.19
CHEMBL5271038 1 7.01
CHEMBL5285688 1 6.78
CHEMBL5277957 1 6.16
CHEMBL5273751 1 5.33
CHEMBL5291018 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5281842 IC50 = 18.7 nM 7.73
CHEMBL5267263 IC50 = 19.4 nM 7.71
CHEMBL5282503 IC50 = 30.9 nM 7.51
CHEMBL5286386 IC50 = 40.4 nM 7.39
CHEMBL5272194 IC50 = 62.7 nM 7.20
CHEMBL5273393 IC50 = 65.0 nM 7.19
CHEMBL5271038 IC50 = 98.3 nM 7.01
CHEMBL5285688 IC50 = 165.0 nM 6.78
CHEMBL5277957 IC50 = 695.0 nM 6.16
CHEMBL5273751 IC50 = 4720.0 nM 5.33
CHEMBL5291018 IC50 = 4830.0 nM 5.32