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Assay Detail

CHEMBL3418331

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

Functional
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
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
EC50 27 6.27 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236715 1 9.05
CHEMBL308954 ETRAVIRINE 4.0 1 8.40
CHEMBL223228 EFAVIRENZ 4.0 1 8.22
CHEMBL129 ZIDOVUDINE 4.0 1 8.15
CHEMBL3330984 1 7.30
CHEMBL3415138 1 6.58
CHEMBL57 NEVIRAPINE 4.0 1 6.51
CHEMBL3415142 1 6.50
CHEMBL929 DELAVIRDINE MESYLATE 4.0 1 6.27
CHEMBL3415150 1 6.06
CHEMBL3415148 1 6.01
CHEMBL3415139 1 5.89
CHEMBL141 LAMIVUDINE 4.0 1 5.66
CHEMBL3415143 1 5.64
CHEMBL3415149 1 5.40
CHEMBL3415151 1 5.34
CHEMBL3415134 1 5.19
CHEMBL3415146 1 5.14
CHEMBL3415140 1 5.04
CHEMBL3415144 1 4.72
CHEMBL1460 DIDANOSINE 4.0 1 4.64
CHEMBL3415147 1 -
CHEMBL3415145 1 -
CHEMBL3415141 1 -
CHEMBL3415137 1 -
CHEMBL3415136 1 -
CHEMBL3415135 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236715 EC50 = 0.9 nM 9.05
CHEMBL308954 ETRAVIRINE EC50 = 4.0 nM 8.40
CHEMBL223228 EFAVIRENZ EC50 = 6.0 nM 8.22
CHEMBL129 ZIDOVUDINE EC50 = 7.0 nM 8.15
CHEMBL3330984 EC50 = 50.0 nM 7.30
CHEMBL3415138 EC50 = 260.0 nM 6.58
CHEMBL57 NEVIRAPINE EC50 = 310.0 nM 6.51
CHEMBL3415142 EC50 = 320.0 nM 6.50
CHEMBL929 DELAVIRDINE MESYLATE EC50 = 540.0 nM 6.27
CHEMBL3415150 EC50 = 870.0 nM 6.06
CHEMBL3415148 EC50 = 980.0 nM 6.01
CHEMBL3415139 EC50 = 1300.0 nM 5.89
CHEMBL141 LAMIVUDINE EC50 = 2200.0 nM 5.66
CHEMBL3415143 EC50 = 2300.0 nM 5.64
CHEMBL3415149 EC50 = 4000.0 nM 5.40
CHEMBL3415151 EC50 = 4600.0 nM 5.34
CHEMBL3415134 EC50 = 6500.0 nM 5.19
CHEMBL3415146 EC50 = 7200.0 nM 5.14
CHEMBL3415140 EC50 = 9200.0 nM 5.04
CHEMBL3415144 EC50 = 19000.0 nM 4.72
CHEMBL1460 DIDANOSINE EC50 = 23000.0 nM 4.64
CHEMBL3415147 EC50 > 28000.0 nM -
CHEMBL3415145 EC50 > 13000.0 nM -
CHEMBL3415141 EC50 > 12000.0 nM -
CHEMBL3415137 EC50 > 57000.0 nM -
CHEMBL3415136 EC50 > 156000.0 nM -
CHEMBL3415135 EC50 > 5300.0 nM -