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Assay Detail

CHEMBL5609481

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

Functional
Antiviral activity against HIV-1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
16
Total Activities
16
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

Structure-based discovery of novel piperidine-biphenyl-DAPY derivatives as non-nucleoside reverse transcriptase inhibitors featuring improved potency, safety, and selectivity: From piperazine-biphenyl-DAPYs to piperidine-biphenyl-DAPYs.
Huang WJ, Pannecouque C, De Clercq E, Wang S, Chen FE.
Eur J Med Chem (2024) 276 : 116668 -116668
PubMed 38996652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 8.10
CHEMBL308954 ETRAVIRINE 4.0 1 7.80
CHEMBL129 ZIDOVUDINE 4.0 1 7.68
CHEMBL5612014 1 7.42
CHEMBL5614187 1 7.32
CHEMBL5612952 1 7.29
CHEMBL5612553 1 7.18
CHEMBL5613123 1 7.17
CHEMBL5613254 1 7.14
CHEMBL5613183 1 7.12
CHEMBL5612205 1 7.00
CHEMBL5613811 1 6.93
CHEMBL5612529 1 6.87
CHEMBL5612186 1 6.80
CHEMBL5612631 1 6.70
CHEMBL57 NEVIRAPINE 4.0 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ EC50 = 8.0 nM 8.10
CHEMBL308954 ETRAVIRINE EC50 = 16.0 nM 7.80
CHEMBL129 ZIDOVUDINE EC50 = 21.0 nM 7.68
CHEMBL5612014 EC50 = 38.0 nM 7.42
CHEMBL5614187 EC50 = 48.0 nM 7.32
CHEMBL5612952 EC50 = 51.0 nM 7.29
CHEMBL5612553 EC50 = 66.0 nM 7.18
CHEMBL5613123 EC50 = 67.0 nM 7.17
CHEMBL5613254 EC50 = 72.0 nM 7.14
CHEMBL5613183 EC50 = 76.0 nM 7.12
CHEMBL5612205 EC50 = 99.0 nM 7.00
CHEMBL5613811 EC50 = 118.0 nM 6.93
CHEMBL5612529 EC50 = 134.0 nM 6.87
CHEMBL5612186 EC50 = 158.0 nM 6.80
CHEMBL5612631 EC50 = 202.0 nM 6.70
CHEMBL57 NEVIRAPINE EC50 = 7148.0 nM 5.15