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Assay Detail

CHEMBL797524

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Binding
Inhibition of HIV-1 reverse transcriptase using rCdG as template and dGTP as substrate
ChEMBL ↗
65
Total Activities
65
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

Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
Bell FW, Cantrell AS, Högberg M, Jaskunas SR, Johansson NG, Jordan CL, Kinnick MD, Lind P, Morin JM, Noréen R.
J Med Chem (1995) 38 : 4929 -4936
PubMed 8523406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.90 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88677 — — 1 9.00
CHEMBL398766 — — 1 8.52
CHEMBL399976 — — 1 8.35
CHEMBL400547 — — 1 8.30
CHEMBL254007 — — 1 8.22
CHEMBL253369 — — 1 8.22
CHEMBL252137 — — 1 8.22
CHEMBL438146 — — 1 8.00
CHEMBL252136 — — 1 8.00
CHEMBL250438 — — 1 8.00
CHEMBL317356 — — 1 7.82
CHEMBL39999 TROVIRDINE 2.0 1 7.82
CHEMBL316796 — — 1 7.70
CHEMBL398765 — — 1 7.52
CHEMBL252135 — — 1 7.52
CHEMBL147749 — — 1 7.52
CHEMBL254201 — — 1 7.40
CHEMBL400546 — — 1 7.30
CHEMBL254414 — — 1 7.22
CHEMBL253994 — — 1 7.22
CHEMBL254207 — — 1 7.10
CHEMBL400685 — — 1 7.05
CHEMBL268871 L-697661 — 1 7.00
CHEMBL254628 — — 1 7.00
CHEMBL254413 — — 1 6.82
CHEMBL400733 — — 1 6.82
CHEMBL253995 — — 1 6.82
CHEMBL254839 — — 1 6.70
CHEMBL254415 — — 1 6.70
CHEMBL398764 — — 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88677 — IC50 = 1.0 nM 9.00
CHEMBL398766 — IC50 = 3.0 nM 8.52
CHEMBL399976 — IC50 = 4.5 nM 8.35
CHEMBL400547 — IC50 = 5.0 nM 8.30
CHEMBL254007 — IC50 = 6.0 nM 8.22
CHEMBL253369 — IC50 = 6.0 nM 8.22
CHEMBL252137 — IC50 = 6.0 nM 8.22
CHEMBL438146 — IC50 = 10.0 nM 8.00
CHEMBL252136 — IC50 = 10.0 nM 8.00
CHEMBL250438 — IC50 = 10.0 nM 8.00
CHEMBL317356 — IC50 = 15.0 nM 7.82
CHEMBL39999 TROVIRDINE IC50 = 15.0 nM 7.82
CHEMBL316796 — IC50 = 20.0 nM 7.70
CHEMBL252135 — IC50 = 30.0 nM 7.52
CHEMBL398765 — IC50 = 30.0 nM 7.52
CHEMBL147749 — IC50 = 30.0 nM 7.52
CHEMBL254201 — IC50 = 40.0 nM 7.40
CHEMBL400546 — IC50 = 50.0 nM 7.30
CHEMBL254414 — IC50 = 60.0 nM 7.22
CHEMBL253994 — IC50 = 60.0 nM 7.22
CHEMBL254207 — IC50 = 80.0 nM 7.10
CHEMBL400685 — IC50 = 90.0 nM 7.05
CHEMBL268871 L-697661 IC50 = 100.0 nM 7.00
CHEMBL254628 — IC50 = 100.0 nM 7.00
CHEMBL253995 — IC50 = 150.0 nM 6.82
CHEMBL400733 — IC50 = 150.0 nM 6.82
CHEMBL254413 — IC50 = 150.0 nM 6.82
CHEMBL254839 — IC50 = 200.0 nM 6.70
CHEMBL254415 — IC50 = 200.0 nM 6.70
CHEMBL398764 — IC50 = 200.0 nM 6.70
CHEMBL147099 — IC50 = 200.0 nM 6.70
CHEMBL145709 — IC50 = 200.0 nM 6.70
CHEMBL148106 — IC50 = 200.0 nM 6.70
CHEMBL293498 — IC50 = 200.0 nM 6.70
CHEMBL57 NEVIRAPINE IC50 = 200.0 nM 6.70
CHEMBL401167 — IC50 = 200.0 nM 6.70
CHEMBL399069 — IC50 = 350.0 nM 6.46
CHEMBL254206 — IC50 = 350.0 nM 6.46
CHEMBL254416 — IC50 = 400.0 nM 6.40
CHEMBL144136 — IC50 = 450.0 nM 6.35
CHEMBL410771 — IC50 = 550.0 nM 6.26
CHEMBL102957 — IC50 = 600.0 nM 6.22
CHEMBL254836 — IC50 = 600.0 nM 6.22
CHEMBL359410 — IC50 = 650.0 nM 6.19
CHEMBL33981 — IC50 = 900.0 nM 6.05
CHEMBL253996 — IC50 = 1000.0 nM 6.00
CHEMBL147375 — IC50 = 1100.0 nM 5.96
CHEMBL400684 — IC50 = 1100.0 nM 5.96
CHEMBL145897 — IC50 = 1200.0 nM 5.92
CHEMBL317866 — IC50 = 1500.0 nM 5.82