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Assay Detail

CHEMBL4195355

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Functional
Antiviral activity against HIV-1 LAI infected in human MT2 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
Ghosh AK, R Nyalapatla P, Kovela S, Rao KV, Brindisi M, Osswald HL, Amano M, Aoki M, Agniswamy J, Wang YF, Weber IT, Mitsuya H.
J Med Chem (2018) 61 : 4561 -4577
PubMed 29763303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.30 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4207145 1 10.64
CHEMBL4214453 1 10.57
CHEMBL4218875 1 9.05
CHEMBL4211505 1 8.85
CHEMBL1323 DARUNAVIR 4.0 1 8.49
CHEMBL4218164 1 8.05
CHEMBL4210992 1 7.68
CHEMBL114 SAQUINAVIR 4.0 1 7.68
CHEMBL4213229 1 7.54
CHEMBL4205056 1 7.51
CHEMBL4217920 1 6.89
CHEMBL4214741 1 6.61
CHEMBL4215950 1 -
CHEMBL4206617 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4207145 IC50 = 0.023 nM 10.64
CHEMBL4214453 IC50 = 0.027 nM 10.57
CHEMBL4218875 IC50 = 0.9 nM 9.05
CHEMBL4211505 IC50 = 1.4 nM 8.85
CHEMBL1323 DARUNAVIR IC50 = 3.2 nM 8.49
CHEMBL4218164 IC50 = 9.0 nM 8.05
CHEMBL4210992 IC50 = 21.0 nM 7.68
CHEMBL114 SAQUINAVIR IC50 = 21.0 nM 7.68
CHEMBL4213229 IC50 = 29.0 nM 7.54
CHEMBL4205056 IC50 = 31.0 nM 7.51
CHEMBL4217920 IC50 = 130.0 nM 6.89
CHEMBL4214741 IC50 = 248.0 nM 6.61
CHEMBL4215950 IC50 > 1000.0 nM -
CHEMBL4206617 IC50 > 1000.0 nM -