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Assay Detail

CHEMBL4179250

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Functional
Antiviral activity against HIV2 ROD 3B infected in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 2
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 2 (CHEMBL380)
Type ORGANISM
Organism Human immunodeficiency virus 2

Publication

1-Hydroxypyrido[2,3-d]pyrimidin-2(1H)-ones as novel selective HIV integrase inhibitors obtained via privileged substructure-based compound libraries.
Gao P, Zhang L, Sun L, Huang T, Tan J, Zhang J, Zhou Z, Zhao T, Menéndez-Arias L, Pannecouque C, Clercq E, Zhan P, Liu X.
Bioorg Med Chem (2017) 25 : 5779 -5789
PubMed 28951095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.46 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 8.42
CHEMBL254316 RALTEGRAVIR 4.0 1 7.96
CHEMBL518520 RALTEGRAVIR POTASSIUM 4.0 1 7.80
CHEMBL4218534 1 5.55
CHEMBL4217571 1 4.84
CHEMBL4215971 1 4.16
CHEMBL4217679 1 -
CHEMBL4211952 1 -
CHEMBL4204847 1 -
CHEMBL4209720 1 -
CHEMBL4211903 1 -
CHEMBL4208084 1 -
CHEMBL4207826 1 -
CHEMBL4213875 1 -
CHEMBL4207034 1 -
CHEMBL4210132 1 -
CHEMBL4210823 1 -
CHEMBL4211950 1 -
CHEMBL4214520 1 -
CHEMBL4209924 1 -
CHEMBL4217288 1 -
CHEMBL4212898 1 -
CHEMBL4217053 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR EC50 = 3.8 nM 8.42
CHEMBL254316 RALTEGRAVIR EC50 = 11.0 nM 7.96
CHEMBL518520 RALTEGRAVIR POTASSIUM EC50 = 16.0 nM 7.80
CHEMBL4218534 EC50 = 2820.0 nM 5.55
CHEMBL4217571 EC50 = 14600.0 nM 4.84
CHEMBL4215971 EC50 = 69400.0 nM 4.16
CHEMBL4217679 EC50 > 21800.0 nM -
CHEMBL4211952 EC50 > 22300.0 nM -
CHEMBL4204847 EC50 > 22400.0 nM -
CHEMBL4209720 EC50 > 17800.0 nM -
CHEMBL4211903 EC50 > 24000.0 nM -
CHEMBL4208084 EC50 > 25100.0 nM -
CHEMBL4207826 EC50 > 239200.0 nM -
CHEMBL4213875 EC50 > 275100.0 nM -
CHEMBL4207034 EC50 > 264600.0 nM -
CHEMBL4210132 EC50 > 273300.0 nM -
CHEMBL4210823 EC50 > 239300.0 nM -
CHEMBL4211950 EC50 > 2700.0 nM -
CHEMBL4214520 EC50 > 1100.0 nM -
CHEMBL4209924 EC50 > 23700.0 nM -
CHEMBL4217288 EC50 > 24700.0 nM -
CHEMBL4212898 EC50 > 24100.0 nM -
CHEMBL4217053 EC50 > 24900.0 nM -