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Assay Detail

CHEMBL800589

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Binding
Inhibitory concentration against HIV-1 wild type Reverse transcriptase (RT)
ChEMBL ↗
68
Total Activities
68
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 non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
Proudfoot JR, Hargrave KD, Kapadia SR, Patel UR, Grozinger KG, McNeil DW, Cullen E, Cardozo M, Tong L, Kelly TA.
J Med Chem (1995) 38 : 4830 -4838
PubMed 7490732 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 6.97 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142837 — — 1 8.00
CHEMBL144744 — — 1 8.00
CHEMBL342771 — — 1 7.75
CHEMBL145237 — — 1 7.70
CHEMBL144326 — — 1 7.70
CHEMBL145199 — — 1 7.70
CHEMBL343007 — — 1 7.70
CHEMBL356744 — — 1 7.70
CHEMBL342103 — — 1 7.70
CHEMBL144852 — — 1 7.52
CHEMBL144522 — — 1 7.52
CHEMBL81319 — — 1 7.52
CHEMBL145397 — — 1 7.40
CHEMBL144145 — — 1 7.40
CHEMBL37628 — — 1 7.40
CHEMBL144851 — — 1 7.40
CHEMBL344289 — — 1 7.40
CHEMBL142659 — — 1 7.30
CHEMBL422123 — — 1 7.30
CHEMBL142853 — — 1 7.22
CHEMBL145322 — — 1 7.16
CHEMBL357221 — — 1 7.16
CHEMBL15411 — — 1 7.16
CHEMBL144035 — — 1 7.16
CHEMBL343883 — — 1 7.16
CHEMBL288336 — — 1 7.10
CHEMBL57 NEVIRAPINE 4.0 1 7.10
CHEMBL341847 — — 1 7.05
CHEMBL358947 — — 1 7.05
CHEMBL343625 — — 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142837 — IC50 = 10.0 nM 8.00
CHEMBL144744 — IC50 = 10.0 nM 8.00
CHEMBL342771 — IC50 = 18.0 nM 7.75
CHEMBL145237 — IC50 = 20.0 nM 7.70
CHEMBL144326 — IC50 = 20.0 nM 7.70
CHEMBL145199 — IC50 = 20.0 nM 7.70
CHEMBL343007 — IC50 = 20.0 nM 7.70
CHEMBL356744 — IC50 = 20.0 nM 7.70
CHEMBL342103 — IC50 = 20.0 nM 7.70
CHEMBL144852 — IC50 = 30.0 nM 7.52
CHEMBL144522 — IC50 = 30.0 nM 7.52
CHEMBL81319 — IC50 = 30.0 nM 7.52
CHEMBL37628 — IC50 = 40.0 nM 7.40
CHEMBL144145 — IC50 = 40.0 nM 7.40
CHEMBL145397 — IC50 = 40.0 nM 7.40
CHEMBL144851 — IC50 = 40.0 nM 7.40
CHEMBL344289 — IC50 = 40.0 nM 7.40
CHEMBL142659 — IC50 = 50.0 nM 7.30
CHEMBL422123 — IC50 = 50.0 nM 7.30
CHEMBL142853 — IC50 = 60.0 nM 7.22
CHEMBL145322 — IC50 = 70.0 nM 7.16
CHEMBL357221 — IC50 = 70.0 nM 7.16
CHEMBL15411 — IC50 = 70.0 nM 7.16
CHEMBL144035 — IC50 = 70.0 nM 7.16
CHEMBL343883 — IC50 = 70.0 nM 7.16
CHEMBL288336 — IC50 = 80.0 nM 7.10
CHEMBL57 NEVIRAPINE IC50 = 80.0 nM 7.10
CHEMBL341847 — IC50 = 90.0 nM 7.05
CHEMBL358947 — IC50 = 90.0 nM 7.05
CHEMBL343625 — IC50 = 90.0 nM 7.05
CHEMBL422659 — IC50 = 90.0 nM 7.05
CHEMBL144820 — IC50 = 90.0 nM 7.05
CHEMBL357183 — IC50 = 100.0 nM 7.00
CHEMBL146550 — IC50 = 100.0 nM 7.00
CHEMBL144653 — IC50 = 100.0 nM 7.00
CHEMBL356998 — IC50 = 110.0 nM 6.96
CHEMBL144652 — IC50 = 110.0 nM 6.96
CHEMBL288305 — IC50 = 120.0 nM 6.92
CHEMBL143107 — IC50 = 120.0 nM 6.92
CHEMBL37343 — IC50 = 130.0 nM 6.89
CHEMBL356779 — IC50 = 130.0 nM 6.89
CHEMBL145193 — IC50 = 140.0 nM 6.85
CHEMBL344288 — IC50 = 140.0 nM 6.85
CHEMBL355918 — IC50 = 150.0 nM 6.82
CHEMBL144290 — IC50 = 150.0 nM 6.82
CHEMBL435030 — IC50 = 150.0 nM 6.82
CHEMBL144773 — IC50 = 180.0 nM 6.75
CHEMBL145736 — IC50 = 180.0 nM 6.75
CHEMBL342068 — IC50 = 190.0 nM 6.72
CHEMBL342056 — IC50 = 220.0 nM 6.66