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Assay Detail

CHEMBL5053571

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to hexameric C-terminal His-tagged HIV1 NL4-3 capsid protein A14C/E45C/W184A/M185A mutant expressed in Escherichia coli BL21 codon plus (DE3)RIL assessed as dissociation constant by SPR analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Rapid Optimization of the Metabolic Stability of a Human Immunodeficiency Virus Type-1 Capsid Inhibitor Using a Multistep Computational Workflow.
Meuser ME, Reddy PAN, Dick A, Maurancy JM, Salvino JM, Cocklin S.
J Med Chem (2021) 64 : 3747 -3766
PubMed 33750123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 6.94 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088963 1 7.60
CHEMBL5080573 1 7.36
CHEMBL1229713 1 7.21
CHEMBL5091904 1 7.02
CHEMBL5080202 1 6.86
CHEMBL5076825 1 6.72
CHEMBL5087414 1 6.47
CHEMBL5079461 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088963 Kd = 25.0 nM 7.60
CHEMBL5080573 Kd = 43.9 nM 7.36
CHEMBL1229713 Kd = 61.5 nM 7.21
CHEMBL5091904 Kd = 95.4 nM 7.02
CHEMBL5080202 Kd = 139.0 nM 6.86
CHEMBL5076825 Kd = 189.0 nM 6.72
CHEMBL5087414 Kd = 337.0 nM 6.47
CHEMBL5079461 Kd = 494.0 nM 6.31