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Assay Detail

CHEMBL683816

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

Functional
Inhibitory activity against NNI-resistant HIV-1 strain A17 with Y181C,K103N mutation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Expert

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
Venkatachalam TK, Sudbeck EA, Mao C, Uckun FM.
Bioorg Med Chem Lett (2000) 10 : 2071 -2074
PubMed 10999473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.05 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432526 1 5.57
CHEMBL417737 1 5.24
CHEMBL302866 1 5.09
CHEMBL294743 1 5.00
CHEMBL292339 1 4.99
CHEMBL295585 1 4.39
CHEMBL57 NEVIRAPINE 4.0 1 -
CHEMBL39999 TROVIRDINE 2.0 1 -
CHEMBL593 DELAVIRDINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432526 IC50 = 2700.0 nM 5.57
CHEMBL417737 IC50 = 5800.0 nM 5.24
CHEMBL302866 IC50 = 8200.0 nM 5.09
CHEMBL294743 IC50 = 10000.0 nM 5.00
CHEMBL292339 IC50 = 10200.0 nM 4.99
CHEMBL295585 IC50 = 41000.0 nM 4.39
CHEMBL57 NEVIRAPINE IC50 > 100000.0 nM -
CHEMBL39999 TROVIRDINE IC50 > 100000.0 nM -
CHEMBL593 DELAVIRDINE IC50 > 100000.0 nM -