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Assay Detail

CHEMBL805260

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

Functional
The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type SW480
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Protein Tat (CHEMBL4609)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus type 1 group M subtype B (isolate PCV12)(HIV-1)

Publication

Keto/enol epoxy steroids as HIV-1 Tat inhibitors: structure-activity relationships and pharmacophore localization.
Michne WF, Schroeder JD, Bailey TR, Neumann HC, Cooke D, Young DC, Hughes JV, Kingsley SD, Ryan KA, Putz HS.
J Med Chem (1995) 38 : 3197 -3206
PubMed 7650672 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.96 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137917 1 5.58
CHEMBL3137919 1 5.58
CHEMBL3137916 1 5.57
CHEMBL109492 1 5.55
CHEMBL3137910 1 5.44
CHEMBL91609 1 5.40
CHEMBL323490 1 5.35
CHEMBL320506 1 5.16
CHEMBL2373330 1 5.08
CHEMBL3137920 1 5.08
CHEMBL108427 1 5.00
CHEMBL3137913 1 4.99
CHEMBL3137911 1 4.84
CHEMBL3137914 1 4.81
CHEMBL107878 1 4.78
CHEMBL108485 1 4.67
CHEMBL3138234 1 4.61
CHEMBL111446 1 4.59
CHEMBL111424 1 4.50
CHEMBL323217 1 4.49
CHEMBL325765 1 4.47
CHEMBL110573 1 4.47
CHEMBL320265 1 4.14
CHEMBL326009 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137917 IC50 = 2600.0 nM 5.58
CHEMBL3137919 IC50 = 2600.0 nM 5.58
CHEMBL3137916 IC50 = 2700.0 nM 5.57
CHEMBL109492 IC50 = 2800.0 nM 5.55
CHEMBL3137910 IC50 = 3600.0 nM 5.44
CHEMBL91609 IC50 = 4000.0 nM 5.40
CHEMBL323490 IC50 = 4500.0 nM 5.35
CHEMBL320506 IC50 = 7000.0 nM 5.16
CHEMBL2373330 IC50 = 8400.0 nM 5.08
CHEMBL3137920 IC50 = 8400.0 nM 5.08
CHEMBL108427 IC50 = 9900.0 nM 5.00
CHEMBL3137913 IC50 = 10300.0 nM 4.99
CHEMBL3137911 IC50 = 14300.0 nM 4.84
CHEMBL3137914 IC50 = 15400.0 nM 4.81
CHEMBL107878 IC50 = 16500.0 nM 4.78
CHEMBL108485 IC50 = 21400.0 nM 4.67
CHEMBL3138234 IC50 = 24500.0 nM 4.61
CHEMBL111446 IC50 = 25700.0 nM 4.59
CHEMBL111424 IC50 = 31700.0 nM 4.50
CHEMBL323217 IC50 = 32100.0 nM 4.49
CHEMBL325765 IC50 = 33500.0 nM 4.47
CHEMBL110573 IC50 = 34000.0 nM 4.47
CHEMBL320265 IC50 = 72000.0 nM 4.14
CHEMBL326009 IC50 = 278000.0 nM -