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Assay Detail

CHEMBL2185500

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of HIV1 integrase strand transfer activity using [32P]-labeled linear oligonucleotide substrate
20
Total Activities
20
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 Autocuration

Target

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

Publication

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
Zeng LF, Wang Y, Kazemi R, Xu S, Xu ZL, Sanchez TW, Yang LM, Debnath B, Odde S, Xie H, Zheng YT, Ding J, Neamati N, Long YQ.
J Med Chem (2012) 55 : 9492 -9509
PubMed 23098137 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.93 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180591 1 6.70
CHEMBL2180587 1 6.70
CHEMBL414850 1 6.52
CHEMBL2180589 1 6.52
CHEMBL2180590 1 6.52
CHEMBL2180599 1 6.30
CHEMBL2180586 1 6.16
CHEMBL2180585 1 6.16
CHEMBL2180588 1 6.00
CHEMBL2180600 1 4.89
CHEMBL2180601 1 4.51
CHEMBL2180593 1 4.16
CHEMBL2180594 1 -
CHEMBL2180592 1 -
CHEMBL2180595 1 -
CHEMBL2180596 1 -
CHEMBL2180597 1 -
CHEMBL2180598 1 -
CHEMBL2180571 1 -
CHEMBL2180572 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180591 IC50 = 200.0 nM 6.70
CHEMBL2180587 IC50 = 200.0 nM 6.70
CHEMBL414850 IC50 = 300.0 nM 6.52
CHEMBL2180589 IC50 = 300.0 nM 6.52
CHEMBL2180590 IC50 = 300.0 nM 6.52
CHEMBL2180599 IC50 = 500.0 nM 6.30
CHEMBL2180586 IC50 = 700.0 nM 6.16
CHEMBL2180585 IC50 = 700.0 nM 6.16
CHEMBL2180588 IC50 = 1000.0 nM 6.00
CHEMBL2180600 IC50 = 13000.0 nM 4.89
CHEMBL2180601 IC50 = 31000.0 nM 4.51
CHEMBL2180593 IC50 = 69000.0 nM 4.16
CHEMBL2180594 IC50 > 100000.0 nM -
CHEMBL2180592 IC50 > 100000.0 nM -
CHEMBL2180595 IC50 > 111000.0 nM -
CHEMBL2180596 IC50 > 111000.0 nM -
CHEMBL2180597 IC50 > 100000.0 nM -
CHEMBL2180598 IC50 > 100000.0 nM -
CHEMBL2180571 IC50 > 100000.0 nM -
CHEMBL2180572 IC50 > 100000.0 nM -