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Assay Detail

CHEMBL4332382

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

Functional
Antiviral activity against HIV1 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
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
EC50 16 6.54 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2364608 DORAVIRINE 4.0 1 7.82
CHEMBL4448359 1 6.71
CHEMBL223228 EFAVIRENZ 4.0 1 6.61
CHEMBL4467417 1 6.46
CHEMBL141 LAMIVUDINE 4.0 1 5.11
CHEMBL4461473 1 -
CHEMBL4577434 1 -
CHEMBL4469538 1 -
CHEMBL4579228 1 -
CHEMBL4550743 1 -
CHEMBL4582364 1 -
CHEMBL4530139 1 -
CHEMBL4434794 1 -
CHEMBL4453611 1 -
CHEMBL4576491 1 -
CHEMBL4471313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2364608 DORAVIRINE EC50 = 15.0 nM 7.82
CHEMBL4448359 EC50 = 196.0 nM 6.71
CHEMBL223228 EFAVIRENZ EC50 = 244.0 nM 6.61
CHEMBL4467417 EC50 = 343.0 nM 6.46
CHEMBL141 LAMIVUDINE EC50 = 7770.0 nM 5.11
CHEMBL4461473 EC50 > 234000.0 nM -
CHEMBL4577434 EC50 > 231000.0 nM -
CHEMBL4469538 EC50 > 41900.0 nM -
CHEMBL4579228 EC50 > 133000.0 nM -
CHEMBL4550743 EC50 > 111000.0 nM -
CHEMBL4582364 EC50 > 183000.0 nM -
CHEMBL4530139 EC50 > 254000.0 nM -
CHEMBL4434794 EC50 > 82300.0 nM -
CHEMBL4453611 EC50 > 269000.0 nM -
CHEMBL4576491 EC50 > 87900.0 nM -
CHEMBL4471313 EC50 > 112000.0 nM -