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Assay Detail

CHEMBL802600

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Binding
Inhibitory activity against HIV-1 Y181C reverse transcriptase.
ChEMBL ↗
51
Total Activities
51
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

Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
Klunder JM, Hoermann M, Cywin CL, David E, Brickwood JR, Schwartz R, Barringer KJ, Pauletti D, Shih CK, Erickson DA, Sorge CL, Joseph DP, Hattox SE, Adams J, Grob PM.
J Med Chem (1998) 41 : 2960 -2971
PubMed 9685235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.44 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101845 — — 1 7.52
CHEMBL101946 — — 1 7.16
CHEMBL102113 — — 1 7.16
CHEMBL100934 — — 1 7.10
CHEMBL100833 — — 1 7.10
CHEMBL103953 — — 1 7.05
CHEMBL319091 — — 1 6.96
CHEMBL321544 — — 1 6.92
CHEMBL101412 — — 1 6.89
CHEMBL100136 — — 1 6.85
CHEMBL327938 — — 1 6.85
CHEMBL101501 — — 1 6.85
CHEMBL102192 — — 1 6.82
CHEMBL421210 — — 1 6.82
CHEMBL318952 — — 1 6.80
CHEMBL318982 — — 1 6.75
CHEMBL322869 — — 1 6.70
CHEMBL100056 — — 1 6.64
CHEMBL330416 — — 1 6.60
CHEMBL318635 — — 1 6.60
CHEMBL327744 — — 1 6.55
CHEMBL319032 — — 1 6.55
CHEMBL101998 — — 1 6.54
CHEMBL101944 — — 1 6.50
CHEMBL330602 — — 1 6.44
CHEMBL102960 — — 1 6.43
CHEMBL328848 — — 1 6.36
CHEMBL102163 — — 1 6.34
CHEMBL101938 — — 1 6.32
CHEMBL103716 — — 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101845 — IC50 = 30.0 nM 7.52
CHEMBL101946 — IC50 = 70.0 nM 7.16
CHEMBL102113 — IC50 = 70.0 nM 7.16
CHEMBL100934 — IC50 = 80.0 nM 7.10
CHEMBL100833 — IC50 = 80.0 nM 7.10
CHEMBL103953 — IC50 = 90.0 nM 7.05
CHEMBL319091 — IC50 = 110.0 nM 6.96
CHEMBL321544 — IC50 = 120.0 nM 6.92
CHEMBL101412 — IC50 = 130.0 nM 6.89
CHEMBL100136 — IC50 = 140.0 nM 6.85
CHEMBL327938 — IC50 = 140.0 nM 6.85
CHEMBL101501 — IC50 = 140.0 nM 6.85
CHEMBL102192 — IC50 = 150.0 nM 6.82
CHEMBL421210 — IC50 = 150.0 nM 6.82
CHEMBL318952 — IC50 = 160.0 nM 6.80
CHEMBL318982 — IC50 = 180.0 nM 6.75
CHEMBL322869 — IC50 = 200.0 nM 6.70
CHEMBL100056 — IC50 = 230.0 nM 6.64
CHEMBL330416 — IC50 = 250.0 nM 6.60
CHEMBL318635 — IC50 = 250.0 nM 6.60
CHEMBL327744 — IC50 = 280.0 nM 6.55
CHEMBL319032 — IC50 = 280.0 nM 6.55
CHEMBL101998 — IC50 = 290.0 nM 6.54
CHEMBL101944 — IC50 = 320.0 nM 6.50
CHEMBL330602 — IC50 = 360.0 nM 6.44
CHEMBL102960 — IC50 = 370.0 nM 6.43
CHEMBL328848 — IC50 = 440.0 nM 6.36
CHEMBL102163 — IC50 = 460.0 nM 6.34
CHEMBL101938 — IC50 = 480.0 nM 6.32
CHEMBL103716 — IC50 = 520.0 nM 6.28
CHEMBL101834 — IC50 = 560.0 nM 6.25
CHEMBL100629 — IC50 = 580.0 nM 6.24
CHEMBL100352 — IC50 = 740.0 nM 6.13
CHEMBL330597 — IC50 = 1170.0 nM 5.93
CHEMBL101670 — IC50 = 1180.0 nM 5.93
CHEMBL318720 — IC50 = 1200.0 nM 5.92
CHEMBL319762 — IC50 = 1600.0 nM 5.80
CHEMBL103593 — IC50 = 1700.0 nM 5.77
CHEMBL318646 — IC50 = 2160.0 nM 5.67
CHEMBL321765 — IC50 = 2500.0 nM 5.60
CHEMBL318562 — IC50 = 2880.0 nM 5.54
CHEMBL100844 — IC50 = 2900.0 nM 5.54
CHEMBL318343 — IC50 = 3800.0 nM 5.42
CHEMBL317072 — IC50 = 6100.0 nM 5.21
CHEMBL71766 — IC50 >> 1000.0 nM -
CHEMBL100568 — IC50 > 1000.0 nM -
CHEMBL102056 — IC50 > 1000.0 nM -
CHEMBL100968 — IC50 > 1000.0 nM -
CHEMBL329938 — IC50 > 1000.0 nM -
CHEMBL99844 — IC50 > 1000.0 nM -