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Assay Detail

CHEMBL752872

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Binding
Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 with a Y181C mutation in RT (reverse transcriptase)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
Venkatachalam TK, Sudbeck EA, Mao C, Uckun FM.
Bioorg Med Chem Lett (2001) 11 : 523 -528
PubMed 11229762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.06 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116474 1 7.32
CHEMBL144604 1 7.16
CHEMBL149161 1 6.22
CHEMBL146770 1 6.05
CHEMBL148698 1 5.70
CHEMBL151773 1 5.68
CHEMBL356247 1 5.66
CHEMBL149100 1 5.41
CHEMBL345996 1 5.36
CHEMBL358280 1 -
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116474 IC50 = 48.0 nM 7.32
CHEMBL144604 IC50 = 70.0 nM 7.16
CHEMBL149161 IC50 = 600.0 nM 6.22
CHEMBL146770 IC50 = 900.0 nM 6.05
CHEMBL148698 IC50 = 2000.0 nM 5.70
CHEMBL151773 IC50 = 2100.0 nM 5.68
CHEMBL356247 IC50 = 2200.0 nM 5.66
CHEMBL149100 IC50 = 3900.0 nM 5.41
CHEMBL345996 IC50 = 4400.0 nM 5.36
CHEMBL358280 IC50 > 100000.0 nM -
CHEMBL57 NEVIRAPINE IC50 > 100000.0 nM -