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Assay Detail

CHEMBL902989

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Functional
Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay
ChEMBL ↗
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type U-87MG ATCC
Confidence 1 — Organism
Curated By Intermediate

Target

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

Publication

Design and synthesis of human immunodeficiency virus entry inhibitors: sulfonamide as an isostere for the alpha-ketoamide group.
Lu RJ, Tucker JA, Zinevitch T, Kirichenko O, Konoplev V, Kuznetsova S, Sviridov S, Pickens J, Tandel S, Brahmachary E, Yang Y, Wang J, Freel S, Fisher S, Sullivan A, Zhou J, Stanfield-Oakley S, Greenberg M, Bolognesi D, Bray B, Koszalka B, Jeffs P, Khasanov A, Ma YA, Jeffries C, Liu C, Proskurina T, Zhu T, Chucholowski A, Li R, Sexton C.
J Med Chem (2007) 50 : 6535 -6544
PubMed 18052117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 6.16 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399421 — — 1 8.30
CHEMBL239424 — — 1 8.15
CHEMBL337301 — — 1 8.10
CHEMBL238103 — — 1 7.58
CHEMBL391722 — — 1 7.57
CHEMBL442078 — — 1 7.52
CHEMBL238266 — — 1 7.44
CHEMBL238115 — — 1 7.27
CHEMBL239423 — — 1 7.10
CHEMBL238111 — — 1 7.10
CHEMBL237677 — — 1 6.85
CHEMBL235966 — — 1 6.82
CHEMBL392758 — — 1 6.82
CHEMBL392576 — — 1 6.80
CHEMBL238108 — — 1 6.70
CHEMBL235971 — — 1 6.70
CHEMBL391846 — — 1 6.70
CHEMBL428725 — — 1 6.62
CHEMBL394005 — — 1 6.62
CHEMBL236603 — — 1 6.60
CHEMBL238113 — — 1 6.52
CHEMBL391847 — — 1 6.43
CHEMBL391499 — — 1 6.38
CHEMBL238100 — — 1 6.37
CHEMBL237859 — — 1 6.30
CHEMBL238109 — — 1 6.30
CHEMBL393331 — — 1 6.30
CHEMBL240049 — — 1 6.28
CHEMBL393719 — — 1 6.28
CHEMBL236780 — — 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399421 — IC50 = 5.0 nM 8.30
CHEMBL239424 — IC50 = 7.0 nM 8.15
CHEMBL337301 — IC50 = 8.0 nM 8.10
CHEMBL238103 — IC50 = 26.0 nM 7.58
CHEMBL391722 — IC50 = 27.0 nM 7.57
CHEMBL442078 — IC50 = 30.0 nM 7.52
CHEMBL238266 — IC50 = 36.0 nM 7.44
CHEMBL238115 — IC50 = 54.0 nM 7.27
CHEMBL239423 — IC50 = 80.0 nM 7.10
CHEMBL238111 — IC50 = 80.0 nM 7.10
CHEMBL237677 — IC50 = 140.0 nM 6.85
CHEMBL235966 — IC50 = 150.0 nM 6.82
CHEMBL392758 — IC50 = 150.0 nM 6.82
CHEMBL392576 — IC50 = 160.0 nM 6.80
CHEMBL391846 — IC50 = 200.0 nM 6.70
CHEMBL235971 — IC50 = 200.0 nM 6.70
CHEMBL238108 — IC50 = 200.0 nM 6.70
CHEMBL428725 — IC50 = 240.0 nM 6.62
CHEMBL394005 — IC50 = 240.0 nM 6.62
CHEMBL236603 — IC50 = 250.0 nM 6.60
CHEMBL238113 — IC50 = 300.0 nM 6.52
CHEMBL391847 — IC50 = 370.0 nM 6.43
CHEMBL391499 — IC50 = 420.0 nM 6.38
CHEMBL238100 — IC50 = 430.0 nM 6.37
CHEMBL393331 — IC50 = 500.0 nM 6.30
CHEMBL238109 — IC50 = 500.0 nM 6.30
CHEMBL237859 — IC50 = 500.0 nM 6.30
CHEMBL240049 — IC50 = 520.0 nM 6.28
CHEMBL393719 — IC50 = 520.0 nM 6.28
CHEMBL236780 — IC50 = 580.0 nM 6.24
CHEMBL238265 — IC50 = 620.0 nM 6.21
CHEMBL237858 — IC50 = 640.0 nM 6.19
CHEMBL237676 — IC50 = 860.0 nM 6.07
CHEMBL236997 — IC50 = 860.0 nM 6.07
CHEMBL237675 — IC50 = 1100.0 nM 5.96
CHEMBL393332 — IC50 = 1240.0 nM 5.91
CHEMBL429809 — IC50 = 1900.0 nM 5.72
CHEMBL240476 — IC50 = 2300.0 nM 5.64
CHEMBL439564 — IC50 = 2400.0 nM 5.62
CHEMBL238990 — IC50 = 3000.0 nM 5.52
CHEMBL239204 — IC50 = 3300.0 nM 5.48
CHEMBL393585 — IC50 = 3600.0 nM 5.44
CHEMBL235964 — IC50 = 4200.0 nM 5.38
CHEMBL240477 — IC50 = 4600.0 nM 5.34
CHEMBL240688 — IC50 = 4600.0 nM 5.34
CHEMBL392342 — IC50 = 4700.0 nM 5.33
CHEMBL393400 — IC50 = 5400.0 nM 5.27
CHEMBL240063 — IC50 = 8400.0 nM 5.08
CHEMBL429087 — IC50 = 9200.0 nM 5.04
CHEMBL240064 — IC50 = 9100.0 nM 5.04