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Assay Detail

CHEMBL4679105

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Functional
Antiviral activity against wild type HIV-1 infected in human MT4 cells by MTT assay
20
Total Activities
20
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 Autocuration

Target

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

Publication

Discovery of novel HIV-1 integrase-LEDGF/p75 allosteric inhibitors based on a pyridine scaffold forming an intramolecular hydrogen bond.
Sugiyama S,Akiyama T,Taoda Y,Iwaki T,Matsuoka E,Akihisa E,Seki T,Yoshinaga T,Kawasuji T
Bioorg Med Chem Lett (2021) 33 : 127742 -127742
PubMed 33316407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.46 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4742369 1 8.18
CHEMBL4798646 1 8.18
CHEMBL4777060 1 8.08
CHEMBL4787805 1 8.00
CHEMBL4789641 1 7.96
CHEMBL4757346 1 7.96
CHEMBL4798095 1 7.77
CHEMBL4778776 1 7.70
CHEMBL4796197 1 7.68
CHEMBL3259907 BI-224436 1.0 1 7.66
CHEMBL4741337 1 7.50
CHEMBL4790071 1 7.46
CHEMBL4793299 1 7.35
CHEMBL4758161 1 7.21
CHEMBL4754449 1 6.75
CHEMBL4781525 1 6.72
CHEMBL4754803 1 6.66
CHEMBL4786494 1 6.46
CHEMBL4785613 1 6.44
CHEMBL4743299 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4742369 EC50 = 6.6 nM 8.18
CHEMBL4798646 EC50 = 6.6 nM 8.18
CHEMBL4777060 EC50 = 8.3 nM 8.08
CHEMBL4787805 EC50 = 10.0 nM 8.00
CHEMBL4789641 EC50 = 11.0 nM 7.96
CHEMBL4757346 EC50 = 11.0 nM 7.96
CHEMBL4798095 EC50 = 17.0 nM 7.77
CHEMBL4778776 EC50 = 20.0 nM 7.70
CHEMBL4796197 EC50 = 21.0 nM 7.68
CHEMBL3259907 BI-224436 EC50 = 22.0 nM 7.66
CHEMBL4741337 EC50 = 32.0 nM 7.50
CHEMBL4790071 EC50 = 35.0 nM 7.46
CHEMBL4793299 EC50 = 45.0 nM 7.35
CHEMBL4758161 EC50 = 61.0 nM 7.21
CHEMBL4754449 EC50 = 180.0 nM 6.75
CHEMBL4781525 EC50 = 190.0 nM 6.72
CHEMBL4754803 EC50 = 220.0 nM 6.66
CHEMBL4786494 EC50 = 350.0 nM 6.46
CHEMBL4785613 EC50 = 360.0 nM 6.44
CHEMBL4743299 EC50 > 100.0 nM -