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Assay Detail

CHEMBL1831952

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

Binding
Binding affinity to HIV1 reverse transcriptase assessed as L-3'-azido-NTP incorporation in nascent DNA
9
Total Activities
9
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

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

Publication

Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.
Zhang HW, Detorio M, Herman BD, Solomon S, Bassit L, Nettles JH, Obikhod A, Tao SJ, Mellors JW, Sluis-Cremer N, Coats SJ, Schinazi RF.
Eur J Med Chem (2011) 46 : 3832 -3844
PubMed 21700368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 5.64 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230 LAMIVUDINE TRIPHOSPHATE -1.0 1 6.89
CHEMBL1830935 1 6.64
CHEMBL66115 DOXECITINE 2.0 1 5.96
CHEMBL220940 THYMIDINE_TRIPHOSPHATE 1 5.68
CHEMBL1830934 1 5.64
CHEMBL335538 1 5.50
CHEMBL477486 DEOXYGUANOSINE TRIPHOSPHATE 1 5.38
CHEMBL1830933 1 4.82
CHEMBL193952 ZIDOVUDINE TRIPHOSPHATE -1.0 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230 LAMIVUDINE TRIPHOSPHATE Kd = 130.0 nM 6.89
CHEMBL1830935 Kd = 230.0 nM 6.64
CHEMBL66115 DOXECITINE Kd = 1100.0 nM 5.96
CHEMBL220940 THYMIDINE_TRIPHOSPHATE Kd = 2100.0 nM 5.68
CHEMBL1830934 Kd = 2300.0 nM 5.64
CHEMBL335538 Kd = 3200.0 nM 5.50
CHEMBL477486 DEOXYGUANOSINE TRIPHOSPHATE Kd = 4200.0 nM 5.38
CHEMBL1830933 Kd = 15000.0 nM 4.82
CHEMBL193952 ZIDOVUDINE TRIPHOSPHATE Kd = 55000.0 nM 4.26