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Assay Detail

CHEMBL5356170

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

Functional
Anti-HIV activity against drug resistant HIV-1 harboring K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Development of novel S-N<sub>3</sub>-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity.
Ling X, Hao QQ, Huang WJ, Pannecouque C, De Clercq E, Wang S, Chen FE.
Eur J Med Chem (2023) 247 : 115042 -115042
PubMed 36577220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.16 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 7.62
CHEMBL223228 EFAVIRENZ 4.0 1 7.03
CHEMBL5405590 1 5.60
CHEMBL5433611 1 5.48
CHEMBL5411806 1 5.41
CHEMBL5425978 1 5.32
CHEMBL5416641 1 5.22
CHEMBL57 NEVIRAPINE 4.0 1 5.09
CHEMBL5434015 1 5.09
CHEMBL5436998 1 4.85
CHEMBL5430980 1 4.68
CHEMBL5427605 1 4.42
CHEMBL5421659 1 4.29
CHEMBL5395674 1 4.21
CHEMBL374286 1 4.17
CHEMBL5419681 1 4.14
CHEMBL5422267 1 -
CHEMBL5439822 1 -
CHEMBL5429802 1 -
CHEMBL5404627 1 -
CHEMBL5402260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 24.0 nM 7.62
CHEMBL223228 EFAVIRENZ EC50 = 94.0 nM 7.03
CHEMBL5405590 EC50 = 2510.0 nM 5.60
CHEMBL5433611 EC50 = 3300.0 nM 5.48
CHEMBL5411806 EC50 = 3900.0 nM 5.41
CHEMBL5425978 EC50 = 4820.0 nM 5.32
CHEMBL5416641 EC50 = 6030.0 nM 5.22
CHEMBL57 NEVIRAPINE EC50 = 8100.0 nM 5.09
CHEMBL5434015 EC50 = 8200.0 nM 5.09
CHEMBL5436998 EC50 = 14260.0 nM 4.85
CHEMBL5430980 EC50 = 20860.0 nM 4.68
CHEMBL5427605 EC50 = 38220.0 nM 4.42
CHEMBL5421659 EC50 = 51180.0 nM 4.29
CHEMBL5395674 EC50 = 61100.0 nM 4.21
CHEMBL374286 EC50 = 68280.0 nM 4.17
CHEMBL5419681 EC50 = 71560.0 nM 4.14
CHEMBL5422267 EC50 > 387450.0 nM -
CHEMBL5439822 EC50 = 107340.0 nM -
CHEMBL5429802 EC50 > 139080.0 nM -
CHEMBL5404627 EC50 > 153540.0 nM -
CHEMBL5402260 EC50 > 342000.0 nM -