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Assay Detail

CHEMBL4137328

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

Functional
Antiviral activity against ENV pseudotyped CCR5-tropic HIV1 JFRL infected in human HeLa67 cells after 3 days by luciferase reporter gene assay
ChEMBL ↗
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Human immunodeficiency virus 1 (CHEMBL378) ↗
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.
Wang T, Ueda Y, Zhang Z, Yin Z, Matiskella J, Pearce BC, Yang Z, Zheng M, Parker DD, Yamanaka GA, Gong YF, Ho HT, Colonno RJ, Langley DR, Lin PF, Meanwell NA, Kadow JF.
J Med Chem (2018) 61 : 6308 -6327
PubMed 29920093 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 75 9.84 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168284 — — 1 10.82
CHEMBL4162336 — — 1 10.70
CHEMBL4164445 — — 1 10.70
CHEMBL4174437 — — 1 10.70
CHEMBL4167863 — — 1 10.70
CHEMBL4160380 — — 1 10.52
CHEMBL4169420 — — 1 10.52
CHEMBL4172598 — — 1 10.52
CHEMBL4170162 — — 1 10.52
CHEMBL4174663 — — 1 10.52
CHEMBL4175721 — — 1 10.40
CHEMBL4168341 — — 1 10.40
CHEMBL4173034 — — 1 10.40
CHEMBL4172311 — — 1 10.40
CHEMBL4165990 — — 1 10.30
CHEMBL4069670 — — 1 10.30
CHEMBL4167684 — — 1 10.30
CHEMBL4164009 — — 1 10.22
CHEMBL4171621 — — 1 10.22
CHEMBL4160252 — — 1 10.22
CHEMBL4172108 — — 1 10.15
CHEMBL4080382 — — 1 10.15
CHEMBL4164913 — — 1 10.15
CHEMBL4173528 — — 1 10.10
CHEMBL4160454 — — 1 10.10
CHEMBL4170079 — — 1 10.10
CHEMBL4104608 — — 1 10.05
CHEMBL4160874 — — 1 10.05
CHEMBL4171053 — — 1 10.05
CHEMBL4168761 — — 1 10.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168284 — EC50 = 0.015 nM 10.82
CHEMBL4162336 — EC50 = 0.02 nM 10.70
CHEMBL4167863 — EC50 = 0.02 nM 10.70
CHEMBL4164445 — EC50 = 0.02 nM 10.70
CHEMBL4174437 — EC50 = 0.02 nM 10.70
CHEMBL4160380 — EC50 = 0.03 nM 10.52
CHEMBL4169420 — EC50 = 0.03 nM 10.52
CHEMBL4172598 — EC50 = 0.03 nM 10.52
CHEMBL4170162 — EC50 = 0.03 nM 10.52
CHEMBL4174663 — EC50 = 0.03 nM 10.52
CHEMBL4172311 — EC50 = 0.04 nM 10.40
CHEMBL4173034 — EC50 = 0.04 nM 10.40
CHEMBL4168341 — EC50 = 0.04 nM 10.40
CHEMBL4175721 — EC50 = 0.04 nM 10.40
CHEMBL4167684 — EC50 = 0.05 nM 10.30
CHEMBL4165990 — EC50 = 0.05 nM 10.30
CHEMBL4069670 — EC50 = 0.05 nM 10.30
CHEMBL4164009 — EC50 = 0.06 nM 10.22
CHEMBL4171621 — EC50 = 0.06 nM 10.22
CHEMBL4160252 — EC50 = 0.06 nM 10.22
CHEMBL4172108 — EC50 = 0.07 nM 10.15
CHEMBL4080382 — EC50 = 0.07 nM 10.15
CHEMBL4164913 — EC50 = 0.07 nM 10.15
CHEMBL4170079 — EC50 = 0.08 nM 10.10
CHEMBL4173528 — EC50 = 0.08 nM 10.10
CHEMBL4160454 — EC50 = 0.08 nM 10.10
CHEMBL4104608 — EC50 = 0.09 nM 10.05
CHEMBL4160874 — EC50 = 0.09 nM 10.05
CHEMBL4171053 — EC50 = 0.09 nM 10.05
CHEMBL4168761 — EC50 = 0.09 nM 10.05
CHEMBL4168167 — EC50 = 0.09 nM 10.05
CHEMBL3301620 TEMSAVIR EC50 = 0.1 nM 10.00
CHEMBL4160609 — EC50 = 0.1 nM 10.00
CHEMBL4172558 — EC50 = 0.1 nM 10.00
CHEMBL4175067 — EC50 = 0.1 nM 10.00
CHEMBL4168551 — EC50 = 0.11 nM 9.96
CHEMBL4169366 — EC50 = 0.11 nM 9.96
CHEMBL4170256 — EC50 = 0.11 nM 9.96
CHEMBL4175083 — EC50 = 0.11 nM 9.96
CHEMBL4165784 — EC50 = 0.12 nM 9.92
CHEMBL4159942 — EC50 = 0.13 nM 9.89
CHEMBL4162247 — EC50 = 0.13 nM 9.89
CHEMBL4173701 — EC50 = 0.13 nM 9.89
CHEMBL4177071 — EC50 = 0.13 nM 9.89
CHEMBL4167202 — EC50 = 0.14 nM 9.85
CHEMBL4176602 — EC50 = 0.14 nM 9.85
CHEMBL4164235 — EC50 = 0.14 nM 9.85
CHEMBL4177292 — EC50 = 0.16 nM 9.80
CHEMBL4176192 — EC50 = 0.16 nM 9.80
CHEMBL4160831 — EC50 = 0.17 nM 9.77