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Assay Detail

CHEMBL4682691

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

Functional
Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
Xiao T,Tang JF,Meng G,Pannecouque C,Zhu YY,Liu GY,Xu ZQ,Wu FS,Gu SX,Chen FE
Eur J Med Chem (2020) 186 : 111864 -111864
PubMed 31767136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 5.84 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57 NEVIRAPINE 4.0 1 8.49
CHEMBL141 LAMIVUDINE 4.0 1 7.72
CHEMBL223228 EFAVIRENZ 4.0 1 7.12
CHEMBL4747887 1 7.11
CHEMBL4760322 1 6.66
CHEMBL4795358 1 5.72
CHEMBL308954 ETRAVIRINE 4.0 1 5.70
CHEMBL4791463 1 5.58
CHEMBL4753622 1 5.42
CHEMBL4759040 1 5.40
CHEMBL4782911 1 5.31
CHEMBL129 ZIDOVUDINE 4.0 1 5.25
CHEMBL4753117 1 5.24
CHEMBL4789866 1 5.09
CHEMBL4755739 1 5.08
CHEMBL4791987 1 5.05
CHEMBL4753696 1 5.02
CHEMBL4750572 1 5.01
CHEMBL4795491 1 5.00
CHEMBL4755133 1 -
CHEMBL4748035 1 -
CHEMBL4749739 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57 NEVIRAPINE EC50 = 3.2 nM 8.49
CHEMBL141 LAMIVUDINE EC50 = 19.0 nM 7.72
CHEMBL223228 EFAVIRENZ EC50 = 76.0 nM 7.12
CHEMBL4747887 EC50 = 77.0 nM 7.11
CHEMBL4760322 EC50 = 220.0 nM 6.66
CHEMBL4795358 EC50 = 1900.0 nM 5.72
CHEMBL308954 ETRAVIRINE EC50 = 2000.0 nM 5.70
CHEMBL4791463 EC50 = 2600.0 nM 5.58
CHEMBL4753622 EC50 = 3800.0 nM 5.42
CHEMBL4759040 EC50 = 4000.0 nM 5.40
CHEMBL4782911 EC50 = 4900.0 nM 5.31
CHEMBL129 ZIDOVUDINE EC50 = 5600.0 nM 5.25
CHEMBL4753117 EC50 = 5700.0 nM 5.24
CHEMBL4789866 EC50 = 8200.0 nM 5.09
CHEMBL4755739 EC50 = 8300.0 nM 5.08
CHEMBL4791987 EC50 = 8900.0 nM 5.05
CHEMBL4753696 EC50 = 9600.0 nM 5.02
CHEMBL4750572 EC50 = 9800.0 nM 5.01
CHEMBL4795491 EC50 = 10000.0 nM 5.00
CHEMBL4755133 EC50 > 27000.0 nM -
CHEMBL4748035 EC50 > 32000.0 nM -
CHEMBL4749739 EC50 > 5400.0 nM -