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Assay Detail

CHEMBL5122833

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Functional
Antiproliferative activity against human 22Rv1 cells expressing AKR1C3 assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CWR22R
Confidence 1 — Organism
Curated By Autocuration

Target

CWR22R (CHEMBL612657)
Type CELL-LINE
Organism Homo sapiens

Publication

New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the hydroxytriazole scaffold.
Pippione AC, Kilic-Kurt Z, Kovachka S, Sainas S, Rolando B, Denasio E, Pors K, Adinolfi S, Zonari D, Bagnati R, Lolli ML, Spyrakis F, Oliaro-Bosso S, Boschi D.
Eur J Med Chem (2022) 237 : 114366 -114366
PubMed 35447434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.24 4.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191752 1 4.47
CHEMBL5170149 1 4.30
CHEMBL5194388 1 4.28
CHEMBL5174744 1 4.26
CHEMBL5187723 1 4.24
CHEMBL5175151 1 4.24
CHEMBL5170401 1 4.23
CHEMBL5172658 1 4.19
CHEMBL5206583 1 4.17
CHEMBL5204156 1 4.12
CHEMBL4174786 1 4.09
CHEMBL5183881 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191752 IC50 = 33800.0 nM 4.47
CHEMBL5170149 IC50 = 50100.0 nM 4.30
CHEMBL5194388 IC50 = 52060.0 nM 4.28
CHEMBL5174744 IC50 = 54810.0 nM 4.26
CHEMBL5187723 IC50 = 57940.0 nM 4.24
CHEMBL5175151 IC50 = 58180.0 nM 4.24
CHEMBL5170401 IC50 = 59010.0 nM 4.23
CHEMBL5172658 IC50 = 64950.0 nM 4.19
CHEMBL5206583 IC50 = 67540.0 nM 4.17
CHEMBL5204156 IC50 = 75740.0 nM 4.12
CHEMBL4174786 IC50 = 81400.0 nM 4.09
CHEMBL5183881 IC50 > 100000.0 nM -