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Assay Detail

CHEMBL798357

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

Binding
Ability to inhibit HIV-1 Reverse Transcriptase (RT) using an rC-dG template/primer
18
Total Activities
18
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 of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Tucker TJ, Lyle TA, Wiscount CM, Britcher SF, Young SD, Sanders WM, Lumma WC, Goldman ME, O'Brien JA, Ball RG.
J Med Chem (1994) 37 : 2437 -2444
PubMed 7520079 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.22 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL78882 1 8.04
CHEMBL81227 1 7.97
CHEMBL79526 1 7.96
CHEMBL309896 1 7.92
CHEMBL82764 1 7.89
CHEMBL80064 1 7.75
CHEMBL268871 L-697661 1 7.72
CHEMBL314012 1 7.71
CHEMBL311996 1 7.63
CHEMBL309462 1 7.19
CHEMBL79403 1 7.16
CHEMBL57 NEVIRAPINE 4.0 1 7.14
CHEMBL310306 1 6.89
CHEMBL82481 1 6.57
CHEMBL79696 1 6.35
CHEMBL309696 1 5.82
CHEMBL311050 1 5.03
CHEMBL82662 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL78882 IC50 = 9.2 nM 8.04
CHEMBL81227 IC50 = 10.8 nM 7.97
CHEMBL79526 IC50 = 10.9 nM 7.96
CHEMBL309896 IC50 = 12.0 nM 7.92
CHEMBL82764 IC50 = 12.8 nM 7.89
CHEMBL80064 IC50 = 17.7 nM 7.75
CHEMBL268871 L-697661 IC50 = 19.0 nM 7.72
CHEMBL314012 IC50 = 19.6 nM 7.71
CHEMBL311996 IC50 = 23.2 nM 7.63
CHEMBL309462 IC50 = 64.5 nM 7.19
CHEMBL79403 IC50 = 70.0 nM 7.16
CHEMBL57 NEVIRAPINE IC50 = 73.0 nM 7.14
CHEMBL310306 IC50 = 130.0 nM 6.89
CHEMBL82481 IC50 = 270.0 nM 6.57
CHEMBL79696 IC50 = 450.0 nM 6.35
CHEMBL309696 IC50 = 1500.0 nM 5.82
CHEMBL311050 IC50 = 9300.0 nM 5.03
CHEMBL82662 IC50 > 10000.0 nM -