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Assay Detail

CHEMBL4725952

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Binding
Binding affinity to wild type HIV1 integrase G140S/Q148H mutant
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Integrase (CHEMBL4296304)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors.
Patel M,Naidu BN,Dicker I,Higley H,Lin Z,Terry B,Protack T,Krystal M,Jenkins S,Parker D,Panja C,Rampulla R,Mathur A,Meanwell NA,Walker MA
Bioorg Med Chem (2020) 28 : 115541 -115541
PubMed 32389483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.94 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786078 1 8.10
CHEMBL4779601 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786078 Ki = 8.0 nM 8.10
CHEMBL4779601 Ki = 17.0 nM 7.77