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Assay Detail

CHEMBL768319

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

Binding
Concentration required to inhibit Y181C type RNA dependent DNA polymerase.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 3 — Cell-line / Tissue
Curated By Intermediate

Target

Nucleic Acid (CHEMBL345)
Type NUCLEIC-ACID

Publication

Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs.
Genin MJ, Poel TJ, Yagi Y, Biles C, Althaus I, Keiser BJ, Kopta LA, Friis JM, Reusser F, Adams WJ, Olmsted RA, Voorman RL, Thomas RC, Romero DL.
J Med Chem (1996) 39 : 5267 -5275
PubMed 8978855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.79 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338435 1 6.29
CHEMBL151565 1 6.10
CHEMBL124338 1 5.96
CHEMBL151955 1 5.70
CHEMBL151316 1 5.70
CHEMBL358754 1 5.43
CHEMBL147224 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338435 IC50 = 510.0 nM 6.29
CHEMBL151565 IC50 = 800.0 nM 6.10
CHEMBL124338 IC50 = 1100.0 nM 5.96
CHEMBL151955 IC50 = 2000.0 nM 5.70
CHEMBL151316 IC50 = 2000.0 nM 5.70
CHEMBL358754 IC50 = 3700.0 nM 5.43
CHEMBL147224 IC50 = 4800.0 nM 5.32