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Assay Detail

CHEMBL701116

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Functional
Inhibitory activity against 3'-processing of DNA by HIV-1 integrase
ChEMBL ↗
67
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Coumarin-based inhibitors of HIV integrase.
Zhao H, Neamati N, Hong H, Mazumder A, Wang S, Sunder S, Milne GW, Pommier Y, Burke TR.
J Med Chem (1997) 40 : 242 -249
PubMed 9003523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 4.73 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32711 — — 1 6.43
CHEMBL293914 — — 2 5.82
CHEMBL315955 — — 2 5.54
CHEMBL83786 3,3'-(Ferrocenomethylene)bis[4-hydroxycoumarin] — 2 5.44
CHEMBL309502 — — 1 5.38
CHEMBL284384 — — 3 5.26
CHEMBL314013 — — 1 5.16
CHEMBL84518 — — 3 5.10
CHEMBL81797 — — 3 5.07
CHEMBL310293 — — 3 5.00
CHEMBL80104 — — 3 4.85
CHEMBL310188 — — 1 4.76
CHEMBL316387 — — 3 4.72
CHEMBL81144 — — 3 4.54
CHEMBL309505 — — 3 4.47
CHEMBL82974 — — 2 4.47
CHEMBL82742 — — 1 4.45
CHEMBL313509 — — 2 4.37
CHEMBL80018 — — 2 4.35
CHEMBL312727 — — 1 4.33
CHEMBL82696 — — 2 4.32
CHEMBL81935 — — 2 4.27
CHEMBL310585 — — 2 4.21
CHEMBL82828 — — 1 4.09
CHEMBL84340 — — 2 4.08
CHEMBL82228 — — 2 4.00
CHEMBL312008 — — 2 4.00
CHEMBL262114 — — 3 -
CHEMBL83968 — — 3 -
CHEMBL32810 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32711 — IC50 = 370.0 nM 6.43
CHEMBL293914 — IC50 = 1500.0 nM 5.82
CHEMBL293914 — IC50 = 2000.0 nM 5.70
CHEMBL315955 — IC50 = 2900.0 nM 5.54
CHEMBL315955 — IC50 = 3000.0 nM 5.52
CHEMBL83786 3,3'-(Ferrocenomethylene)bis[4-hydroxycoumarin] IC50 = 3600.0 nM 5.44
CHEMBL309502 — IC50 = 4200.0 nM 5.38
CHEMBL284384 — IC50 = 5500.0 nM 5.26
CHEMBL284384 — IC50 = 7000.0 nM 5.16
CHEMBL314013 — IC50 = 7000.0 nM 5.16
CHEMBL84518 — IC50 = 8000.0 nM 5.10
CHEMBL81797 — IC50 = 8500.0 nM 5.07
CHEMBL284384 — IC50 = 9200.0 nM 5.04
CHEMBL310293 — IC50 = 10000.0 nM 5.00
CHEMBL84518 — IC50 = 10000.0 nM 5.00
CHEMBL310293 — IC50 = 10000.0 nM 5.00
CHEMBL310293 — IC50 = 11000.0 nM 4.96
CHEMBL83786 3,3'-(Ferrocenomethylene)bis[4-hydroxycoumarin] IC50 = 11000.0 nM 4.96
CHEMBL84518 — IC50 = 11000.0 nM 4.96
CHEMBL80104 — IC50 = 14000.0 nM 4.85
CHEMBL80104 — IC50 = 15000.0 nM 4.82
CHEMBL80104 — IC50 = 16000.0 nM 4.80
CHEMBL310188 — IC50 = 17200.0 nM 4.76
CHEMBL316387 — IC50 = 19000.0 nM 4.72
CHEMBL81797 — IC50 = 19000.0 nM 4.72
CHEMBL316387 — IC50 = 20000.0 nM 4.70
CHEMBL81797 — IC50 = 20000.0 nM 4.70
CHEMBL316387 — IC50 = 20000.0 nM 4.70
CHEMBL81144 — IC50 = 29000.0 nM 4.54
CHEMBL309505 — IC50 = 34000.0 nM 4.47
CHEMBL82974 — IC50 = 34000.0 nM 4.47
CHEMBL81144 — IC50 = 35000.0 nM 4.46
CHEMBL82742 — IC50 = 35700.0 nM 4.45
CHEMBL82974 — IC50 = 40000.0 nM 4.40
CHEMBL81144 — IC50 = 40000.0 nM 4.40
CHEMBL313509 — IC50 = 43000.0 nM 4.37
CHEMBL313509 — IC50 = 43400.0 nM 4.36
CHEMBL80018 — IC50 = 45000.0 nM 4.35
CHEMBL80018 — IC50 = 46000.0 nM 4.34
CHEMBL312727 — IC50 = 46300.0 nM 4.33
CHEMBL82696 — IC50 = 48000.0 nM 4.32
CHEMBL81935 — IC50 = 54000.0 nM 4.27
CHEMBL309505 — IC50 = 54000.0 nM 4.27
CHEMBL81935 — IC50 = 58000.0 nM 4.24
CHEMBL310585 — IC50 = 62000.0 nM 4.21
CHEMBL82696 — IC50 = 66000.0 nM 4.18
CHEMBL309505 — IC50 = 75000.0 nM 4.12
CHEMBL82828 — IC50 = 80600.0 nM 4.09
CHEMBL84340 — IC50 = 84000.0 nM 4.08
CHEMBL84340 — IC50 = 94000.0 nM 4.03