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Assay Detail

CHEMBL797529

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

Binding
Inhibition of wild-type HIV-1 Reverse transcriptase.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.
Högberg M, Engelhardt P, Vrang L, Zhang H.
Bioorg Med Chem Lett (2000) 10 : 265 -268
PubMed 10698450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.87 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88677 1 9.00
CHEMBL88840 1 8.52
CHEMBL91624 1 8.52
CHEMBL328258 1 8.52
CHEMBL91332 1 8.40
CHEMBL36424 1 8.40
CHEMBL88710 1 8.22
CHEMBL88729 1 8.10
CHEMBL88397 1 8.00
CHEMBL398891 THIOUREA, N-(5-BROMO-2-PYRIDINYL)-N'-(2-(2-CHLORO-3-ETHOXY-6-FLUOROPHENYL)ETHYL)- 2.0 1 7.92
CHEMBL254201 1 7.40
CHEMBL89195 1 7.33
CHEMBL88966 1 7.27
CHEMBL313998 1 7.10
CHEMBL539427 1 6.75
CHEMBL91942 1 6.40
CHEMBL414887 1 -
CHEMBL90204 1 -
CHEMBL89082 1 -
CHEMBL327777 1 -
CHEMBL91473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88677 IC50 = 1.0 nM 9.00
CHEMBL88840 IC50 = 3.0 nM 8.52
CHEMBL91624 IC50 = 3.0 nM 8.52
CHEMBL328258 IC50 = 3.0 nM 8.52
CHEMBL91332 IC50 = 4.0 nM 8.40
CHEMBL36424 IC50 = 4.0 nM 8.40
CHEMBL88710 IC50 = 6.0 nM 8.22
CHEMBL88729 IC50 = 8.0 nM 8.10
CHEMBL88397 IC50 = 10.0 nM 8.00
CHEMBL398891 THIOUREA, N-(5-BROMO-2-PYRIDINYL)-N'-(2-(2-CHLORO-3-ETHOXY-6-FLUOROPHENYL)ETHYL)- IC50 = 12.0 nM 7.92
CHEMBL254201 IC50 = 40.0 nM 7.40
CHEMBL89195 IC50 = 47.0 nM 7.33
CHEMBL88966 IC50 = 54.0 nM 7.27
CHEMBL313998 IC50 = 80.0 nM 7.10
CHEMBL539427 IC50 = 180.0 nM 6.75
CHEMBL91942 IC50 = 400.0 nM 6.40
CHEMBL414887 IC50 > 10000.0 nM -
CHEMBL90204 IC50 > 10000.0 nM -
CHEMBL89082 IC50 > 10000.0 nM -
CHEMBL327777 IC50 < 27.0 nM -
CHEMBL91473 IC50 < 25.0 nM -