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Assay Detail

CHEMBL945967

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Functional
Antiviral activity against HIV1 3B in MT2 cells after 5 days
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Intermediate

Target

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

Publication

Tricyclic HIV integrase inhibitors: potent and orally bioavailable C5-aza analogs.
Jin H, Wright M, Pastor R, Mish M, Metobo S, Jabri S, Lansdown R, Cai R, Pyun P, Tsiang M, Chen X, Kim CU.
Bioorg Med Chem Lett (2008) 18 : 1388 -1391
PubMed 18207398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.21 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254524 1 8.85
CHEMBL254318 1 8.77
CHEMBL402290 1 8.51
CHEMBL209854 1 8.47
CHEMBL254316 RALTEGRAVIR 4.0 1 8.22
CHEMBL254522 1 8.00
CHEMBL254523 1 7.51
CHEMBL254317 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254524 EC50 = 1.4 nM 8.85
CHEMBL254318 EC50 = 1.7 nM 8.77
CHEMBL402290 EC50 = 3.1 nM 8.51
CHEMBL209854 EC50 = 3.4 nM 8.47
CHEMBL254316 RALTEGRAVIR EC50 = 6.0 nM 8.22
CHEMBL254522 EC50 = 10.0 nM 8.00
CHEMBL254523 EC50 = 31.0 nM 7.51
CHEMBL254317 EC50 = 47.0 nM 7.33