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Assay Detail

CHEMBL833080

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Functional
Inhibitory activity against HIV-1 mutant strain 188L
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
Benjahad A, Courté K, Guillemont J, Mabire D, Coupa S, Poncelet A, Csoka I, Andries K, Pauwels R, de Béthune MP, Monneret C, Bisagni E, Nguyen CH, Grierson DS.
J Med Chem (2004) 47 : 5501 -5514
PubMed 15481987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 5.79 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182921 — — 1 7.40
CHEMBL366692 — — 1 6.82
CHEMBL361069 — — 1 6.82
CHEMBL223228 EFAVIRENZ 4.0 1 6.82
CHEMBL190941 — — 1 6.82
CHEMBL183249 — — 1 6.82
CHEMBL185715 — — 1 6.82
CHEMBL189458 — — 1 6.70
CHEMBL182580 — — 1 6.60
CHEMBL181747 — — 1 6.60
CHEMBL338047 — — 1 6.60
CHEMBL188878 — — 1 6.51
CHEMBL188941 — — 1 6.51
CHEMBL363952 — — 1 6.41
CHEMBL182725 — — 1 6.41
CHEMBL188580 — — 1 6.41
CHEMBL188877 — — 1 6.30
CHEMBL364122 — — 1 6.20
CHEMBL184294 — — 1 6.20
CHEMBL185487 — — 1 6.20
CHEMBL188223 — — 1 6.10
CHEMBL182846 — — 1 6.10
CHEMBL364403 — — 1 6.10
CHEMBL434518 — — 1 6.00
CHEMBL187786 — — 1 6.00
CHEMBL189760 — — 1 5.80
CHEMBL361479 — — 1 5.80
CHEMBL187305 — — 1 5.80
CHEMBL188547 — — 1 5.70
CHEMBL186390 — — 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182921 — IC50 = 40.0 nM 7.40
CHEMBL366692 — IC50 = 150.0 nM 6.82
CHEMBL361069 — IC50 = 150.0 nM 6.82
CHEMBL223228 EFAVIRENZ IC50 = 150.0 nM 6.82
CHEMBL190941 — IC50 = 150.0 nM 6.82
CHEMBL183249 — IC50 = 150.0 nM 6.82
CHEMBL185715 — IC50 = 150.0 nM 6.82
CHEMBL189458 — IC50 = 200.0 nM 6.70
CHEMBL182580 — IC50 = 250.0 nM 6.60
CHEMBL181747 — IC50 = 250.0 nM 6.60
CHEMBL338047 — IC50 = 250.0 nM 6.60
CHEMBL188878 — IC50 = 310.0 nM 6.51
CHEMBL188941 — IC50 = 310.0 nM 6.51
CHEMBL188580 — IC50 = 390.0 nM 6.41
CHEMBL363952 — IC50 = 390.0 nM 6.41
CHEMBL182725 — IC50 = 390.0 nM 6.41
CHEMBL188877 — IC50 = 500.0 nM 6.30
CHEMBL364122 — IC50 = 630.0 nM 6.20
CHEMBL184294 — IC50 = 630.0 nM 6.20
CHEMBL185487 — IC50 = 630.0 nM 6.20
CHEMBL188223 — IC50 = 790.0 nM 6.10
CHEMBL182846 — IC50 = 790.0 nM 6.10
CHEMBL364403 — IC50 = 790.0 nM 6.10
CHEMBL434518 — IC50 = 1000.0 nM 6.00
CHEMBL187786 — IC50 = 1000.0 nM 6.00
CHEMBL189760 — IC50 = 1580.0 nM 5.80
CHEMBL187305 — IC50 = 1580.0 nM 5.80
CHEMBL361479 — IC50 = 1580.0 nM 5.80
CHEMBL188547 — IC50 = 1990.0 nM 5.70
CHEMBL186390 — IC50 = 1990.0 nM 5.70
CHEMBL189030 — IC50 = 1990.0 nM 5.70
CHEMBL175522 — IC50 = 1990.0 nM 5.70
CHEMBL185865 — IC50 = 2510.0 nM 5.60
CHEMBL188489 — IC50 = 3160.0 nM 5.50
CHEMBL188995 — IC50 = 5010.0 nM 5.30
CHEMBL366120 — IC50 = 7940.0 nM 5.10
CHEMBL188745 — IC50 = 7940.0 nM 5.10
CHEMBL362435 — IC50 = 10000.0 nM 5.00
CHEMBL426242 — IC50 = 10000.0 nM 5.00
CHEMBL182299 — IC50 = 10000.0 nM 5.00
CHEMBL361250 — IC50 = 10000.0 nM 5.00
CHEMBL359749 — IC50 = 10000.0 nM 5.00
CHEMBL181497 — IC50 = 18640.0 nM 4.73
CHEMBL35033 EMIVIRINE IC50 = 39810.0 nM 4.40
CHEMBL181683 — IC50 = 50120.0 nM 4.30
CHEMBL442222 — IC50 = 100000.0 nM 4.00
CHEMBL186129 — IC50 = 100000.0 nM 4.00
CHEMBL57 NEVIRAPINE IC50 = 100000.0 nM 4.00
CHEMBL184934 — IC50 = 100000.0 nM 4.00
CHEMBL185622 — IC50 = 3981000.0 nM -