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Assay Detail

CHEMBL797531

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Binding
Inhibitory effect on wild type HIV- 1 reverse transcriptase using rCdG as template and dGTP as substrate.
16
Total Activities
16
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

Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Sahlberg C, Noréen R, Engelhardt P, Högberg M, Kangasmetsä J, Vrang L, Zhang H.
Bioorg Med Chem Lett (1998) 8 : 1511 -1516
PubMed 9873380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.97 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL37835 1 8.82
CHEMBL37024 1 8.82
CHEMBL37762 1 8.70
CHEMBL38341 1 8.70
CHEMBL287317 1 8.52
CHEMBL38318 1 8.40
CHEMBL36424 1 8.40
CHEMBL37834 1 8.15
CHEMBL35729 1 8.10
CHEMBL37025 1 8.10
CHEMBL39999 TROVIRDINE 2.0 1 7.82
CHEMBL39665 1 7.60
CHEMBL40562 1 7.00
CHEMBL268871 L-697661 1 7.00
CHEMBL35434 1 6.70
CHEMBL57 NEVIRAPINE 4.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL37835 IC50 = 1.5 nM 8.82
CHEMBL37024 IC50 = 1.5 nM 8.82
CHEMBL37762 IC50 = 2.0 nM 8.70
CHEMBL38341 IC50 = 2.0 nM 8.70
CHEMBL287317 IC50 = 3.0 nM 8.52
CHEMBL38318 IC50 = 4.0 nM 8.40
CHEMBL36424 IC50 = 4.0 nM 8.40
CHEMBL37834 IC50 = 7.0 nM 8.15
CHEMBL35729 IC50 = 8.0 nM 8.10
CHEMBL37025 IC50 = 8.0 nM 8.10
CHEMBL39999 TROVIRDINE IC50 = 15.0 nM 7.82
CHEMBL39665 IC50 = 25.0 nM 7.60
CHEMBL40562 IC50 = 100.0 nM 7.00
CHEMBL268871 L-697661 IC50 = 100.0 nM 7.00
CHEMBL35434 IC50 = 200.0 nM 6.70
CHEMBL57 NEVIRAPINE IC50 = 200.0 nM 6.70