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Assay Detail

CHEMBL5113065

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Functional
Antiproliferative activity against human UM-UC-9 cells measured after 7 days by IncuCyte live-cell imaging analysis
19
Total Activities
19
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 Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists <b>BAY-4931</b> and <b>BAY-0069</b>.
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT.
J Med Chem (2022) 65 : 14843 -14863
PubMed 36270630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.28 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191837 1 8.72
CHEMBL5187164 1 8.60
CHEMBL5204936 1 8.55
CHEMBL5206512 1 8.51
CHEMBL5207130 1 8.47
CHEMBL5207464 1 8.28
CHEMBL5184027 1 8.06
CHEMBL5199152 1 8.04
CHEMBL5201278 1 7.28
CHEMBL5179281 1 6.50
CHEMBL5206276 1 6.48
CHEMBL5173312 1 6.45
CHEMBL5183657 1 6.04
CHEMBL5201597 1 5.91
CHEMBL5182665 1 5.43
CHEMBL5201306 1 5.18
CHEMBL5170260 1 -
CHEMBL5186962 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191837 IC50 = 1.9 nM 8.72
CHEMBL5187164 IC50 = 2.5 nM 8.60
CHEMBL5204936 IC50 = 2.8 nM 8.55
CHEMBL5206512 IC50 = 3.1 nM 8.51
CHEMBL5207130 IC50 = 3.4 nM 8.47
CHEMBL5207464 IC50 = 5.3 nM 8.28
CHEMBL5184027 IC50 = 8.8 nM 8.06
CHEMBL5199152 IC50 = 9.2 nM 8.04
CHEMBL5201278 IC50 = 52.0 nM 7.28
CHEMBL5179281 IC50 = 314.0 nM 6.50
CHEMBL5206276 IC50 = 330.0 nM 6.48
CHEMBL5173312 IC50 = 358.0 nM 6.45
CHEMBL5183657 IC50 = 913.0 nM 6.04
CHEMBL5201597 IC50 = 1220.0 nM 5.91
CHEMBL5182665 IC50 = 3710.0 nM 5.43
CHEMBL5201306 IC50 = 6640.0 nM 5.18
CHEMBL5170260 IC50 > 10000.0 nM -
CHEMBL5186962 IC50 > 10000.0 nM -
CHEMBL121 ROSIGLITAZONE IC50 - -