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Assay Detail

CHEMBL833792

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Functional
In vitro inhibitory concentration against HIV-1 Y181C mutant strain
ChEMBL ↗
48
Total Activities
47
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: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
Benjahad A, Croisy M, Monneret C, Bisagni E, Mabire D, Coupa S, Poncelet A, Csoka I, Guillemont J, Meyer C, Andries K, Pauwels R, de Béthune MP, Himmel DM, Das K, Arnold E, Nguyen CH, Grierson DS.
J Med Chem (2005) 48 : 1948 -1964
PubMed 15771439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 5.82 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 8.70
CHEMBL177666 — — 1 7.50
CHEMBL426046 — — 1 7.40
CHEMBL175693 — — 1 7.30
CHEMBL366692 — — 1 7.20
CHEMBL424772 — — 1 7.14
CHEMBL338047 — — 1 7.00
CHEMBL176107 — — 1 6.90
CHEMBL178689 — — 1 6.80
CHEMBL177978 — — 1 6.80
CHEMBL175823 — — 1 6.60
CHEMBL174726 — — 1 6.50
CHEMBL368039 — — 1 6.50
CHEMBL177563 — — 1 6.50
CHEMBL177709 — — 1 6.40
CHEMBL174340 — — 2 6.40
CHEMBL367956 — — 1 6.40
CHEMBL179056 — — 1 6.30
CHEMBL178936 — — 1 6.30
CHEMBL369697 — — 1 6.20
CHEMBL177275 — — 1 6.10
CHEMBL339511 — — 1 6.00
CHEMBL175534 — — 1 5.90
CHEMBL360957 — — 1 5.90
CHEMBL369066 — — 1 5.90
CHEMBL175873 — — 1 5.90
CHEMBL180008 — — 1 5.80
CHEMBL175692 — — 1 5.80
CHEMBL367745 — — 1 5.80
CHEMBL177744 — — 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ IC50 = 2.0 nM 8.70
CHEMBL177666 — IC50 = 32.0 nM 7.50
CHEMBL426046 — IC50 = 40.0 nM 7.40
CHEMBL175693 — IC50 = 50.0 nM 7.30
CHEMBL366692 — IC50 = 63.0 nM 7.20
CHEMBL424772 — IC50 = 72.0 nM 7.14
CHEMBL338047 — IC50 = 100.0 nM 7.00
CHEMBL176107 — IC50 = 126.0 nM 6.90
CHEMBL178689 — IC50 = 160.0 nM 6.80
CHEMBL177978 — IC50 = 158.0 nM 6.80
CHEMBL175823 — IC50 = 251.0 nM 6.60
CHEMBL177563 — IC50 = 316.0 nM 6.50
CHEMBL368039 — IC50 = 316.0 nM 6.50
CHEMBL174726 — IC50 = 316.0 nM 6.50
CHEMBL367956 — IC50 = 398.0 nM 6.40
CHEMBL177709 — IC50 = 398.0 nM 6.40
CHEMBL174340 — IC50 = 398.0 nM 6.40
CHEMBL174340 — IC50 = 398.0 nM 6.40
CHEMBL179056 — IC50 = 501.0 nM 6.30
CHEMBL178936 — IC50 = 501.0 nM 6.30
CHEMBL369697 — IC50 = 631.0 nM 6.20
CHEMBL177275 — IC50 = 794.0 nM 6.10
CHEMBL339511 — IC50 = 1000.0 nM 6.00
CHEMBL175873 — IC50 = 1259.0 nM 5.90
CHEMBL360957 — IC50 = 1259.0 nM 5.90
CHEMBL175534 — IC50 = 1259.0 nM 5.90
CHEMBL369066 — IC50 = 1260.0 nM 5.90
CHEMBL180008 — IC50 = 1585.0 nM 5.80
CHEMBL175692 — IC50 = 1585.0 nM 5.80
CHEMBL367745 — IC50 = 1585.0 nM 5.80
CHEMBL177744 — IC50 = 1995.0 nM 5.70
CHEMBL176207 — IC50 = 2000.0 nM 5.70
CHEMBL175925 — IC50 = 5012.0 nM 5.30
CHEMBL338936 — IC50 = 7943.0 nM 5.10
CHEMBL57 NEVIRAPINE IC50 = 10000.0 nM 5.00
CHEMBL178061 — IC50 = 10000.0 nM 5.00
CHEMBL177491 — IC50 = 10000.0 nM 5.00
CHEMBL424972 — IC50 = 15850.0 nM 4.80
CHEMBL129144 — IC50 = 25120.0 nM 4.60
CHEMBL175655 — IC50 = 39810.0 nM 4.40
CHEMBL366811 — IC50 = 79430.0 nM 4.10
CHEMBL177961 — IC50 = 79430.0 nM 4.10
CHEMBL369460 — IC50 = 100000.0 nM 4.00
CHEMBL179736 — IC50 = 100000.0 nM 4.00
CHEMBL174339 — IC50 = 100000.0 nM 4.00
CHEMBL435522 — IC50 = 100000.0 nM 4.00
CHEMBL128569 — IC50 = 100000.0 nM 4.00
CHEMBL177383 — IC50 = 100000.0 nM 4.00