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Assay Detail

CHEMBL4136670

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

Functional
Antiviral activity against HIV1 infected in GFP expressing human MT4 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% normal human serum
11
Total Activities
11
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 Intermediate

Target

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

Publication

Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Bungard CJ, Williams PD, Schulz J, Wiscount CM, Holloway MK, Loughran HM, Manikowski JJ, Su HP, Bennett DJ, Chang L, Chu XJ, Crespo A, Dwyer MP, Keertikar K, Morriello GJ, Stamford AW, Waddell ST, Zhong B, Hu B, Ji T, Diamond TL, Bahnck-Teets C, Carroll SS, Fay JF, Min X, Morris W, Ballard JE, Miller MD, McCauley JA.
ACS Med Chem Lett (2017) 8 : 1292 -1297
PubMed 29259750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.34 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177355 1 8.55
CHEMBL1323 DARUNAVIR 4.0 1 8.15
CHEMBL1163 ATAZANAVIR 4.0 1 7.92
CHEMBL4173997 1 7.77
CHEMBL4166074 1 7.68
CHEMBL3828743 1 7.57
CHEMBL4163713 1 7.57
CHEMBL4162627 1 7.16
CHEMBL4159254 1 6.28
CHEMBL4170561 1 6.16
CHEMBL4174380 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177355 EC50 = 2.8 nM 8.55
CHEMBL1323 DARUNAVIR EC50 = 7.0 nM 8.15
CHEMBL1163 ATAZANAVIR EC50 = 12.0 nM 7.92
CHEMBL4173997 EC50 = 17.0 nM 7.77
CHEMBL4166074 EC50 = 21.0 nM 7.68
CHEMBL3828743 EC50 = 27.0 nM 7.57
CHEMBL4163713 EC50 = 27.0 nM 7.57
CHEMBL4162627 EC50 = 70.0 nM 7.16
CHEMBL4159254 EC50 = 520.0 nM 6.28
CHEMBL4170561 EC50 = 700.0 nM 6.16
CHEMBL4174380 EC50 = 1200.0 nM 5.92