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Assay Detail

CHEMBL4705077

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Binding
Binding affinity to two PBDs of N36 trimer of gp41 in HIV1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral fusion incubated for 48 hrs by Steady-Glo luciferase assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Cell Type TZM-bl
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Bivalent HIV-1 fusion inhibitors based on peptidomimetics.
Kobayakawa T,Ebihara K,Tsuji K,Kawada T,Fujino M,Honda Y,Ohashi N,Murakami T,Tamamura H
Bioorg Med Chem (2020) 28 : 115812 -115812
PubMed 33157478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.26 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 6.93
CHEMBL440999 1 6.84
CHEMBL2029368 1 5.80
CHEMBL4790610 1 5.77
CHEMBL4751670 1 4.99
CHEMBL4751509 1 4.82
CHEMBL4754444 1 4.77
CHEMBL4762440 1 4.76
CHEMBL4756365 1 4.69
CHEMBL4780685 1 4.64
CHEMBL4789822 1 4.62
CHEMBL4764278 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE IC50 = 118.0 nM 6.93
CHEMBL440999 IC50 = 145.0 nM 6.84
CHEMBL2029368 IC50 = 1600.0 nM 5.80
CHEMBL4790610 IC50 = 1700.0 nM 5.77
CHEMBL4751670 IC50 = 10200.0 nM 4.99
CHEMBL4751509 IC50 = 15000.0 nM 4.82
CHEMBL4754444 IC50 = 17000.0 nM 4.77
CHEMBL4762440 IC50 = 17300.0 nM 4.76
CHEMBL4756365 IC50 = 20500.0 nM 4.69
CHEMBL4780685 IC50 = 22800.0 nM 4.64
CHEMBL4789822 IC50 = 23800.0 nM 4.62
CHEMBL4764278 IC50 = 36300.0 nM 4.44