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Assay Detail

CHEMBL869770

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Binding
Inhibition of strand transfer activity of HIV integrase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
Jin H, Cai RZ, Schacherer L, Jabri S, Tsiang M, Fardis M, Chen X, Chen JM, Kim CU.
Bioorg Med Chem Lett (2006) 16 : 3989 -3992
PubMed 16723225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.54 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209854 1 7.44
CHEMBL414850 1 7.30
CHEMBL209440 1 7.30
CHEMBL211634 1 7.16
CHEMBL212921 1 7.10
CHEMBL211110 1 6.72
CHEMBL379382 1 6.47
CHEMBL378395 1 6.46
CHEMBL210396 1 6.12
CHEMBL377693 1 5.92
CHEMBL209591 1 5.70
CHEMBL211275 1 5.68
CHEMBL212320 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209854 IC50 = 36.0 nM 7.44
CHEMBL414850 IC50 = 50.0 nM 7.30
CHEMBL209440 IC50 = 50.0 nM 7.30
CHEMBL211634 IC50 = 70.0 nM 7.16
CHEMBL212921 IC50 = 80.0 nM 7.10
CHEMBL211110 IC50 = 190.0 nM 6.72
CHEMBL379382 IC50 = 335.0 nM 6.47
CHEMBL378395 IC50 = 350.0 nM 6.46
CHEMBL210396 IC50 = 760.0 nM 6.12
CHEMBL377693 IC50 = 1200.0 nM 5.92
CHEMBL209591 IC50 = 2000.0 nM 5.70
CHEMBL211275 IC50 = 2100.0 nM 5.68
CHEMBL212320 IC50 = 2400.0 nM 5.62