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Assay Detail

CHEMBL1675423

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

Binding
Binding affinity to HIV1 reverse transcriptase
13
Total Activities
13
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

Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.
Sluis-Cremer N, Koontz D, Bassit L, Hernandez-Santiago BI, Detorio M, Rapp KL, Amblard F, Bondada L, Grier J, Coats SJ, Schinazi RF, Mellors JW.
Antimicrob Agents Chemother (2009) 53 : 3715 -3719
PubMed 19596885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 5.62 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230 LAMIVUDINE TRIPHOSPHATE -1.0 1 6.43
CHEMBL560403 DEOXYCYTIDINE TRIPHOSPHATE 1 5.96
CHEMBL193952 ZIDOVUDINE TRIPHOSPHATE -1.0 1 5.70
CHEMBL363559 DEOXYTHYMIDINE_TRIPHOSPHATE 1 5.66
CHEMBL1673189 1 5.64
CHEMBL485652 STAVUDINE TRIPHOSPHATE -1.0 1 5.57
CHEMBL1201384 DDCTP -1.0 1 5.57
CHEMBL1673190 1 5.55
CHEMBL335538 1 5.50
CHEMBL1201395 CARBOVIR 5'-TRIPHOSPHATE, (-)- -1.0 1 5.40
CHEMBL477486 DEOXYGUANOSINE TRIPHOSPHATE 1 5.38
CHEMBL1236349 1 5.37
CHEMBL1383 DDA-TRIPHOSPHATE -1.0 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230 LAMIVUDINE TRIPHOSPHATE Kd = 370.0 nM 6.43
CHEMBL560403 DEOXYCYTIDINE TRIPHOSPHATE Kd = 1100.0 nM 5.96
CHEMBL193952 ZIDOVUDINE TRIPHOSPHATE Kd = 2000.0 nM 5.70
CHEMBL363559 DEOXYTHYMIDINE_TRIPHOSPHATE Kd = 2200.0 nM 5.66
CHEMBL1673189 Kd = 2300.0 nM 5.64
CHEMBL485652 STAVUDINE TRIPHOSPHATE Kd = 2700.0 nM 5.57
CHEMBL1201384 DDCTP Kd = 2700.0 nM 5.57
CHEMBL1673190 Kd = 2800.0 nM 5.55
CHEMBL335538 Kd = 3200.0 nM 5.50
CHEMBL1201395 CARBOVIR 5'-TRIPHOSPHATE, (-)- Kd = 4000.0 nM 5.40
CHEMBL477486 DEOXYGUANOSINE TRIPHOSPHATE Kd = 4200.0 nM 5.38
CHEMBL1236349 Kd = 4300.0 nM 5.37
CHEMBL1383 DDA-TRIPHOSPHATE Kd = 5300.0 nM 5.28