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Assay Detail

CHEMBL798389

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Binding
Concentration required to inhibit the HIV-1 reverse transcriptase activity by 50%.
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
Mai A, Artico M, Sbardella G, Massa S, Novellino E, Greco G, Loi AG, Tramontano E, Marongiu ME, La Colla P.
J Med Chem (1999) 42 : 619 -627
PubMed 10052969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.33 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35033 EMIVIRINE 2.0 1 7.40
CHEMBL83140 — — 1 7.30
CHEMBL87235 — — 1 7.30
CHEMBL87451 — — 1 7.30
CHEMBL87393 — — 1 7.30
CHEMBL157741 — — 1 7.22
CHEMBL156340 — — 1 7.16
CHEMBL309899 — — 1 7.10
CHEMBL312874 — — 1 7.10
CHEMBL160869 — — 1 7.05
CHEMBL156637 — — 1 7.05
CHEMBL156255 — — 1 7.05
CHEMBL154913 — — 1 7.00
CHEMBL347823 — — 1 6.70
CHEMBL345190 — — 1 6.70
CHEMBL157028 — — 1 6.70
CHEMBL155689 — — 1 6.52
CHEMBL157137 — — 1 6.52
CHEMBL57 NEVIRAPINE 4.0 1 6.52
CHEMBL347403 — — 1 6.52
CHEMBL349806 — — 1 6.40
CHEMBL155864 — — 1 6.40
CHEMBL351121 — — 1 6.40
CHEMBL155483 — — 1 6.40
CHEMBL348086 — — 1 6.39
CHEMBL112949 — — 1 6.30
CHEMBL156083 — — 1 6.30
CHEMBL109389 — — 1 6.30
CHEMBL156380 — — 1 6.22
CHEMBL346023 — — 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35033 EMIVIRINE IC50 = 40.0 nM 7.40
CHEMBL83140 — IC50 = 50.0 nM 7.30
CHEMBL87235 — IC50 = 50.0 nM 7.30
CHEMBL87451 — IC50 = 50.0 nM 7.30
CHEMBL87393 — IC50 = 50.0 nM 7.30
CHEMBL157741 — IC50 = 60.0 nM 7.22
CHEMBL156340 — IC50 = 70.0 nM 7.16
CHEMBL309899 — IC50 = 80.0 nM 7.10
CHEMBL312874 — IC50 = 80.0 nM 7.10
CHEMBL160869 — IC50 = 90.0 nM 7.05
CHEMBL156637 — IC50 = 90.0 nM 7.05
CHEMBL156255 — IC50 = 90.0 nM 7.05
CHEMBL154913 — IC50 = 100.0 nM 7.00
CHEMBL157028 — IC50 = 200.0 nM 6.70
CHEMBL347823 — IC50 = 200.0 nM 6.70
CHEMBL345190 — IC50 = 200.0 nM 6.70
CHEMBL155689 — IC50 = 300.0 nM 6.52
CHEMBL157137 — IC50 = 300.0 nM 6.52
CHEMBL57 NEVIRAPINE IC50 = 300.0 nM 6.52
CHEMBL347403 — IC50 = 300.0 nM 6.52
CHEMBL349806 — IC50 = 400.0 nM 6.40
CHEMBL155864 — IC50 = 400.0 nM 6.40
CHEMBL351121 — IC50 = 400.0 nM 6.40
CHEMBL155483 — IC50 = 400.0 nM 6.40
CHEMBL348086 — IC50 = 410.0 nM 6.39
CHEMBL112949 — IC50 = 500.0 nM 6.30
CHEMBL109389 — IC50 = 500.0 nM 6.30
CHEMBL156083 — IC50 = 500.0 nM 6.30
CHEMBL156380 — IC50 = 600.0 nM 6.22
CHEMBL346023 — IC50 = 600.0 nM 6.22
CHEMBL157777 — IC50 = 800.0 nM 6.10
CHEMBL345908 — IC50 = 900.0 nM 6.05
CHEMBL111153 — IC50 = 1000.0 nM 6.00
CHEMBL351323 — IC50 = 1100.0 nM 5.96
CHEMBL156636 — IC50 = 1150.0 nM 5.94
CHEMBL345580 — IC50 = 1150.0 nM 5.94
CHEMBL322898 — IC50 = 1200.0 nM 5.92
CHEMBL160781 — IC50 = 1500.0 nM 5.82
CHEMBL156208 — IC50 = 1500.0 nM 5.82
CHEMBL157349 — IC50 = 1600.0 nM 5.80
CHEMBL114404 — IC50 = 1600.0 nM 5.80
CHEMBL157685 — IC50 = 1700.0 nM 5.77
CHEMBL323573 — IC50 = 1800.0 nM 5.75
CHEMBL422001 — IC50 = 1900.0 nM 5.72
CHEMBL156109 — IC50 = 3000.0 nM 5.52
CHEMBL345128 — IC50 = 4800.0 nM 5.32
CHEMBL347244 — IC50 = 4900.0 nM 5.31
CHEMBL415703 — IC50 = 7400.0 nM 5.13
CHEMBL347255 — IC50 = 8500.0 nM 5.07
CHEMBL316466 — IC50 = 13000.0 nM 4.89