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Assay Detail

CHEMBL3418336

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

Binding
Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA using poly(A) x oligo(dT)15 as template/primer after 1 hr by ELISA
20
Total Activities
20
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

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
Huang B, Liang X, Li C, Chen W, Liu T, Li X, Sun Y, Fu L, Liu H, De Clercq E, Pannecouque C, Zhan P, Liu X.
Eur J Med Chem (2015) 93 : 330 -337
PubMed 25707013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.81 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308954 ETRAVIRINE 4.0 1 6.89
CHEMBL3415144 1 6.77
CHEMBL3415142 1 6.58
CHEMBL3415140 1 6.44
CHEMBL3415138 1 6.40
CHEMBL3415148 1 6.39
CHEMBL3415146 1 6.33
CHEMBL3415134 1 6.09
CHEMBL3415150 1 5.96
CHEMBL3415151 1 5.89
CHEMBL57 NEVIRAPINE 4.0 1 5.62
CHEMBL3415149 1 5.39
CHEMBL3415139 1 5.33
CHEMBL3415145 1 5.26
CHEMBL3415136 1 5.24
CHEMBL3415141 1 5.23
CHEMBL3415147 1 4.96
CHEMBL3415143 1 4.85
CHEMBL3415137 1 4.82
CHEMBL3415135 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308954 ETRAVIRINE IC50 = 130.0 nM 6.89
CHEMBL3415144 IC50 = 170.0 nM 6.77
CHEMBL3415142 IC50 = 260.0 nM 6.58
CHEMBL3415140 IC50 = 360.0 nM 6.44
CHEMBL3415138 IC50 = 400.0 nM 6.40
CHEMBL3415148 IC50 = 410.0 nM 6.39
CHEMBL3415146 IC50 = 470.0 nM 6.33
CHEMBL3415134 IC50 = 820.0 nM 6.09
CHEMBL3415150 IC50 = 1100.0 nM 5.96
CHEMBL3415151 IC50 = 1300.0 nM 5.89
CHEMBL57 NEVIRAPINE IC50 = 2400.0 nM 5.62
CHEMBL3415149 IC50 = 4100.0 nM 5.39
CHEMBL3415139 IC50 = 4700.0 nM 5.33
CHEMBL3415145 IC50 = 5500.0 nM 5.26
CHEMBL3415136 IC50 = 5700.0 nM 5.24
CHEMBL3415141 IC50 = 5900.0 nM 5.23
CHEMBL3415147 IC50 = 11000.0 nM 4.96
CHEMBL3415143 IC50 = 14000.0 nM 4.85
CHEMBL3415137 IC50 = 15000.0 nM 4.82
CHEMBL3415135 IC50 = 334000.0 nM -