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Assay Detail

CHEMBL4332388

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

Binding
Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA
16
Total Activities
16
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

Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Wang Z, Yu Z, Kang D, Zhang J, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem (2019) 27 : 447 -456
PubMed 30606670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.60 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 8.15
CHEMBL2364608 DORAVIRINE 4.0 1 7.72
CHEMBL4448359 1 6.28
CHEMBL57 NEVIRAPINE 4.0 1 6.22
CHEMBL4461473 1 6.03
CHEMBL4471313 1 6.00
CHEMBL4530139 1 5.90
CHEMBL4467417 1 5.90
CHEMBL4577434 1 5.68
CHEMBL4469538 1 4.71
CHEMBL4434794 1 4.52
CHEMBL4579228 1 4.49
CHEMBL4582364 1 4.20
CHEMBL4453611 1 4.14
CHEMBL4576491 1 4.03
CHEMBL4550743 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ IC50 = 7.0 nM 8.15
CHEMBL2364608 DORAVIRINE IC50 = 19.0 nM 7.72
CHEMBL4448359 IC50 = 522.0 nM 6.28
CHEMBL57 NEVIRAPINE IC50 = 595.0 nM 6.22
CHEMBL4461473 IC50 = 930.0 nM 6.03
CHEMBL4471313 IC50 = 1000.0 nM 6.00
CHEMBL4530139 IC50 = 1270.0 nM 5.90
CHEMBL4467417 IC50 = 1250.0 nM 5.90
CHEMBL4577434 IC50 = 2110.0 nM 5.68
CHEMBL4469538 IC50 = 19400.0 nM 4.71
CHEMBL4434794 IC50 = 30100.0 nM 4.52
CHEMBL4579228 IC50 = 32500.0 nM 4.49
CHEMBL4582364 IC50 = 63400.0 nM 4.20
CHEMBL4453611 IC50 = 72000.0 nM 4.14
CHEMBL4576491 IC50 = 92500.0 nM 4.03
CHEMBL4550743 IC50 = 133000.0 nM -