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Assay Detail

CHEMBL3118965

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Binding
Inhibition of HIV wild-type reverse transcriptase by electrochemiluminescence assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
Côté B, Burch JD, Asante-Appiah E, Bayly C, Bédard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschênes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagné S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y.
Bioorg Med Chem Lett (2014) 24 : 917 -922
PubMed 24412110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.07 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 9.00
CHEMBL3115364 1 9.00
CHEMBL308954 ETRAVIRINE 4.0 1 9.00
CHEMBL223228 EFAVIRENZ 4.0 1 8.70
CHEMBL3115366 1 8.70
CHEMBL1928645 1 8.52
CHEMBL3115363 1 8.52
CHEMBL3115352 1 8.52
CHEMBL3115353 1 8.40
CHEMBL3115355 1 8.30
CHEMBL3115367 1 8.30
CHEMBL3115365 1 8.22
CHEMBL3115354 1 8.22
CHEMBL1928643 1 8.15
CHEMBL3115351 1 8.15
CHEMBL3115349 1 8.15
CHEMBL3115348 1 8.15
CHEMBL3115350 1 8.15
CHEMBL3115368 1 8.05
CHEMBL3115358 1 7.96
CHEMBL2364608 DORAVIRINE 4.0 1 7.96
CHEMBL3115356 1 7.80
CHEMBL3115347 1 7.68
CHEMBL3115361 1 7.37
CHEMBL3115362 1 7.30
CHEMBL3115359 1 6.85
CHEMBL3115360 1 6.52
CHEMBL3115357 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE IC50 = 1.0 nM 9.00
CHEMBL3115364 IC50 = 1.0 nM 9.00
CHEMBL308954 ETRAVIRINE IC50 = 1.0 nM 9.00
CHEMBL223228 EFAVIRENZ IC50 = 2.0 nM 8.70
CHEMBL3115366 IC50 = 2.0 nM 8.70
CHEMBL1928645 IC50 = 3.0 nM 8.52
CHEMBL3115363 IC50 = 3.0 nM 8.52
CHEMBL3115352 IC50 = 3.0 nM 8.52
CHEMBL3115353 IC50 = 4.0 nM 8.40
CHEMBL3115355 IC50 = 5.0 nM 8.30
CHEMBL3115367 IC50 = 5.0 nM 8.30
CHEMBL3115365 IC50 = 6.0 nM 8.22
CHEMBL3115354 IC50 = 6.0 nM 8.22
CHEMBL1928643 IC50 = 7.0 nM 8.15
CHEMBL3115351 IC50 = 7.0 nM 8.15
CHEMBL3115349 IC50 = 7.0 nM 8.15
CHEMBL3115348 IC50 = 7.0 nM 8.15
CHEMBL3115350 IC50 = 7.0 nM 8.15
CHEMBL3115368 IC50 = 9.0 nM 8.05
CHEMBL3115358 IC50 = 11.0 nM 7.96
CHEMBL2364608 DORAVIRINE IC50 = 11.0 nM 7.96
CHEMBL3115356 IC50 = 16.0 nM 7.80
CHEMBL3115347 IC50 = 21.0 nM 7.68
CHEMBL3115361 IC50 = 43.0 nM 7.37
CHEMBL3115362 IC50 = 50.0 nM 7.30
CHEMBL3115359 IC50 = 140.0 nM 6.85
CHEMBL3115360 IC50 = 300.0 nM 6.52
CHEMBL3115357 IC50 = 390.0 nM 6.41