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Assay Detail

CHEMBL5507329

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Functional
Antiproliferative activity against human 22Rv1 cells incubated for 72 hrs by SRB assay
18
Total Activities
18
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

Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer.
Pippione AC, Kovachka S, Vigato C, Bertarini L, Mannella I, Sainas S, Rolando B, Denasio E, Piercy-Mycock H, Romalho L, Salladini E, Adinolfi S, Zonari D, Peraldo-Neia C, Chiorino G, Passoni A, Mirza OA, Frydenvang K, Pors K, Lolli ML, Spyrakis F, Oliaro-Bosso S, Boschi D.
Eur J Med Chem (2024) 268 : 116193 -116193
PubMed 38364714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.78 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561463 1 5.70
CHEMBL5559881 1 5.63
CHEMBL5558400 1 5.62
CHEMBL5555217 1 5.09
CHEMBL254328 ABIRATERONE 3.0 1 5.04
CHEMBL5561484 1 4.93
CHEMBL5557454 1 4.78
CHEMBL5532410 1 4.71
CHEMBL5557319 1 4.65
CHEMBL4238437 1 4.57
CHEMBL5557212 1 4.56
CHEMBL5562651 1 4.50
CHEMBL5559780 1 4.43
CHEMBL5517678 1 4.39
CHEMBL5556734 1 4.25
CHEMBL5560443 1 4.24
CHEMBL5566714 1 4.24
CHEMBL4513510 ASP-9521 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561463 IC50 = 2013.0 nM 5.70
CHEMBL5559881 IC50 = 2340.0 nM 5.63
CHEMBL5558400 IC50 = 2390.0 nM 5.62
CHEMBL5555217 IC50 = 8110.0 nM 5.09
CHEMBL254328 ABIRATERONE IC50 = 9090.0 nM 5.04
CHEMBL5561484 IC50 = 11810.0 nM 4.93
CHEMBL5557454 IC50 = 16430.0 nM 4.78
CHEMBL5532410 IC50 = 19600.0 nM 4.71
CHEMBL5557319 IC50 = 22430.0 nM 4.65
CHEMBL4238437 IC50 = 26700.0 nM 4.57
CHEMBL5557212 IC50 = 27330.0 nM 4.56
CHEMBL5562651 IC50 = 31980.0 nM 4.50
CHEMBL5559780 IC50 = 37040.0 nM 4.43
CHEMBL5517678 IC50 = 40960.0 nM 4.39
CHEMBL5556734 IC50 = 56710.0 nM 4.25
CHEMBL5560443 IC50 = 58200.0 nM 4.24
CHEMBL5566714 IC50 = 58270.0 nM 4.24
CHEMBL4513510 ASP-9521 IC50 > 50000.0 nM -