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Assay Detail

CHEMBL857173

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Binding
Inhibitory activity against HIV-1 Integrase (HIV-1-IN)
47
Total Activities
47
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 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

CoMFA and CoMSIA 3D QSAR and docking studies on conformationally-restrained cinnamoyl HIV-1 integrase inhibitors: exploration of a binding mode at the active site.
Buolamwini JK, Assefa H.
J Med Chem (2002) 45 : 841 -852
PubMed 11831895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 4.80 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130911 1 6.70
CHEMBL419981 1 6.70
CHEMBL1161516 1 6.70
CHEMBL129073 1 6.22
CHEMBL129964 1 6.15
CHEMBL339815 1 6.10
CHEMBL129148 1 6.05
CHEMBL276080 1 6.00
CHEMBL341135 1 5.89
CHEMBL131733 1 5.70
CHEMBL132058 1 5.70
CHEMBL129510 1 5.64
CHEMBL83598 1 5.52
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER 1 5.15
CHEMBL131982 1 5.10
CHEMBL353069 1 5.10
CHEMBL133714 BENZYL CAFFEATE 1 5.05
CHEMBL168284 1 4.85
CHEMBL133491 1 4.82
CHEMBL132238 1 4.74
CHEMBL128000 BUTEIN 1 4.70
CHEMBL140 CURCUMIN 3.0 1 4.52
CHEMBL340202 1 4.52
CHEMBL128729 1 4.43
CHEMBL49350 1 4.40
CHEMBL133492 1 4.36
CHEMBL131749 1 4.26
CHEMBL131680 1 4.22
CHEMBL131689 1 4.17
CHEMBL48436 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130911 IC50 = 199.53 nM 6.70
CHEMBL1161516 IC50 = 199.53 nM 6.70
CHEMBL419981 IC50 = 199.53 nM 6.70
CHEMBL129073 IC50 = 602.56 nM 6.22
CHEMBL129964 IC50 = 707.95 nM 6.15
CHEMBL339815 IC50 = 794.33 nM 6.10
CHEMBL129148 IC50 = 891.25 nM 6.05
CHEMBL276080 IC50 = 1000.0 nM 6.00
CHEMBL341135 IC50 = 1288.25 nM 5.89
CHEMBL131733 IC50 = 1995.26 nM 5.70
CHEMBL132058 IC50 = 1995.26 nM 5.70
CHEMBL129510 IC50 = 2290.87 nM 5.64
CHEMBL83598 IC50 = 3019.95 nM 5.52
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER IC50 = 7079.46 nM 5.15
CHEMBL353069 IC50 = 7943.28 nM 5.10
CHEMBL131982 IC50 = 7943.28 nM 5.10
CHEMBL133714 BENZYL CAFFEATE IC50 = 8912.51 nM 5.05
CHEMBL168284 IC50 = 14125.38 nM 4.85
CHEMBL133491 IC50 = 15135.61 nM 4.82
CHEMBL132238 IC50 = 18197.01 nM 4.74
CHEMBL128000 BUTEIN IC50 = 19952.62 nM 4.70
CHEMBL140 CURCUMIN IC50 = 30199.52 nM 4.52
CHEMBL340202 IC50 = 30199.52 nM 4.52
CHEMBL128729 IC50 = 37153.52 nM 4.43
CHEMBL49350 IC50 = 39810.72 nM 4.40
CHEMBL133492 IC50 = 43651.58 nM 4.36
CHEMBL131749 IC50 = 54954.09 nM 4.26
CHEMBL131680 IC50 = 60255.96 nM 4.22
CHEMBL131689 IC50 = 67608.3 nM 4.17
CHEMBL48436 IC50 = 75857.76 nM 4.12
CHEMBL126625 IC50 = 85113.8 nM 4.07
CHEMBL337498 IC50 = 100000.0 nM 4.00
CHEMBL129795 ISOLIQUIRITIGENIN IC50 = 100000.0 nM 4.00
CHEMBL17001 METHYLCAFFEATE IC50 = 100000.0 nM 4.00
CHEMBL133642 IC50 = 100000.0 nM 4.00
CHEMBL170850 IC50 = 100000.0 nM 4.00
CHEMBL442022 IC50 = 100000.0 nM 4.00
CHEMBL17205 CYCLOVALONE IC50 = 100000.0 nM 4.00
CHEMBL129913 IC50 = 100000.0 nM 4.00
CHEMBL128748 DIMETHYLCURCUMIN IC50 = 100000.0 nM 4.00
CHEMBL17347 ETHYL CAFFEATE IC50 = 100000.0 nM 4.00
CHEMBL296582 IC50 = 100000.0 nM 4.00
CHEMBL127028 IC50 = 100000.0 nM 4.00
CHEMBL423698 IC50 = 100000.0 nM 4.00
CHEMBL131678 IC50 = 100000.0 nM 4.00
CHEMBL129134 IC50 = 100000.0 nM 4.00
CHEMBL105350 BISDEMETHOXYCURCUMIN IC50 = 100000.0 nM 4.00