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Assay Detail

CHEMBL689638

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Functional
Equilibrium binding constant at the active site of HIV-1 reverse transcriptase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Effects of fluorine substitution of cytosine analogues on the binding affinity to HIV-1 reverse transcriptase.
Chong Y, Choo H, Chu CK.
Bioorg Med Chem Lett (2004) 14 : 437 -440
PubMed 14698176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 4.64 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341421 EMTRICITABINE 5'-TRIPHOSPHATE -1.0 1 4.92
CHEMBL1230 LAMIVUDINE TRIPHOSPHATE -1.0 1 4.82
CHEMBL341799 1 4.75
CHEMBL136440 1 4.51
CHEMBL138054 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341421 EMTRICITABINE 5'-TRIPHOSPHATE Kd = 12000.0 nM 4.92
CHEMBL1230 LAMIVUDINE TRIPHOSPHATE Kd = 15000.0 nM 4.82
CHEMBL341799 Kd = 18000.0 nM 4.75
CHEMBL136440 Kd = 31000.0 nM 4.51
CHEMBL138054 Kd = 64000.0 nM 4.19