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Assay Detail

CHEMBL701159

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

Binding
Inhibition of HIV-1 integrase by radiolabeled oligonucleotide-based assay integration
27
Total Activities
27
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

Chicoric acid analogues as HIV-1 integrase inhibitors.
Lin Z, Neamati N, Zhao H, Kiryu Y, Turpin JA, Aberham C, Strebel K, Kohn K, Witvrouw M, Pannecouque C, Debyser Z, De Clercq E, Rice WG, Pommier Y, Burke TR.
J Med Chem (1999) 42 : 1401 -1414
PubMed 10212126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.41 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286477 1 6.40
CHEMBL29660 CHICORIC ACID 1 6.30
CHEMBL282731 CICHORIC ACID 1 6.10
CHEMBL416207 1 5.77
CHEMBL30868 1 5.77
CHEMBL284749 1 5.55
CHEMBL30434 1 5.50
CHEMBL34400 1 5.50
CHEMBL30922 1 5.42
CHEMBL29831 1 5.39
CHEMBL30455 1 5.34
CHEMBL29369 1 5.21
CHEMBL31044 1 5.19
CHEMBL31026 1 5.12
CHEMBL31607 1 5.12
CHEMBL31883 1 5.11
CHEMBL32133 1 5.00
CHEMBL281929 1 5.00
CHEMBL416582 1 4.00
CHEMBL286268 1 -
CHEMBL31435 1 -
CHEMBL30698 1 -
CHEMBL31600 1 -
CHEMBL286474 1 -
CHEMBL30488 1 -
CHEMBL30522 1 -
CHEMBL31175 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286477 IC50 = 400.0 nM 6.40
CHEMBL29660 CHICORIC ACID IC50 = 500.0 nM 6.30
CHEMBL282731 CICHORIC ACID IC50 = 800.0 nM 6.10
CHEMBL416207 IC50 = 1700.0 nM 5.77
CHEMBL30868 IC50 = 1700.0 nM 5.77
CHEMBL284749 IC50 = 2800.0 nM 5.55
CHEMBL30434 IC50 = 3200.0 nM 5.50
CHEMBL34400 IC50 = 3200.0 nM 5.50
CHEMBL30922 IC50 = 3800.0 nM 5.42
CHEMBL29831 IC50 = 4100.0 nM 5.39
CHEMBL30455 IC50 = 4600.0 nM 5.34
CHEMBL29369 IC50 = 6200.0 nM 5.21
CHEMBL31044 IC50 = 6500.0 nM 5.19
CHEMBL31026 IC50 = 7500.0 nM 5.12
CHEMBL31607 IC50 = 7600.0 nM 5.12
CHEMBL31883 IC50 = 7800.0 nM 5.11
CHEMBL32133 IC50 = 10100.0 nM 5.00
CHEMBL281929 IC50 = 10000.0 nM 5.00
CHEMBL416582 IC50 = 100000.0 nM 4.00
CHEMBL286268 IC50 > 1000000.0 nM -
CHEMBL31435 IC50 > 333000.0 nM -
CHEMBL30698 IC50 > 1000000.0 nM -
CHEMBL31600 IC50 > 333000.0 nM -
CHEMBL286474 IC50 > 333000.0 nM -
CHEMBL30488 IC50 = 111000.0 nM -
CHEMBL30522 IC50 > 100000.0 nM -
CHEMBL31175 IC50 > 333000.0 nM -