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Assay Detail

CHEMBL5611630

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

Binding
Inhibition of HIV-1 integrase catalytic activity incubated for 1 hrs in absence of LEDGF/p75 by HTRF assay
15
Total Activities
15
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

Quinolinonyl Derivatives as Dual Inhibitors of the HIV-1 Integrase Catalytic Site and Integrase-RNA interactions.
Patacchini E, Madia VN, Albano A, Ruggieri G, Messore A, Ialongo D, Saccoliti F, Scipione L, Cosconati S, Koneru PC, Haney R, Kvaratskhelia M, Di Santo R, Costi R.
ACS Med Chem Lett (2024) 15 : 1533 -1540
PubMed 39291012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.90 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497501 1 7.16
CHEMBL5613927 1 7.11
CHEMBL5613849 1 6.74
CHEMBL5612575 1 6.32
CHEMBL5613097 1 6.13
CHEMBL5613277 1 6.11
CHEMBL5612913 1 6.10
CHEMBL2236593 1 5.63
CHEMBL2236594 1 5.50
CHEMBL5613833 1 5.20
CHEMBL5173288 1 4.44
CHEMBL5172754 1 4.38
CHEMBL5171239 1 -
CHEMBL5613898 1 -
CHEMBL5612322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497501 IC50 = 70.0 nM 7.16
CHEMBL5613927 IC50 = 77.0 nM 7.11
CHEMBL5613849 IC50 = 181.0 nM 6.74
CHEMBL5612575 IC50 = 480.0 nM 6.32
CHEMBL5613097 IC50 = 741.0 nM 6.13
CHEMBL5613277 IC50 = 782.0 nM 6.11
CHEMBL5612913 IC50 = 800.0 nM 6.10
CHEMBL2236593 IC50 = 2340.0 nM 5.63
CHEMBL2236594 IC50 = 3140.0 nM 5.50
CHEMBL5613833 IC50 = 6280.0 nM 5.20
CHEMBL5173288 IC50 = 36500.0 nM 4.44
CHEMBL5172754 IC50 = 41900.0 nM 4.38
CHEMBL5171239 IC50 > 200000.0 nM -
CHEMBL5613898 IC50 > 200000.0 nM -
CHEMBL5612322 IC50 > 200000.0 nM -