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Assay Detail

CHEMBL1040344

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Binding
Inhibition of HIV1 integrase strand transfer activity
ChEMBL ↗
45
Total Activities
45
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

Analysis of binding parameters of HIV-1 integrase inhibitors: correlates of drug inhibition and resistance.
Loizidou EZ, Zeinalipour-Yazdi CD, Christofides T, Kostrikis LG.
Bioorg Med Chem (2009) 17 : 4806 -4818
PubMed 19450984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.60 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572902 — — 1 7.70
CHEMBL573605 — — 1 7.70
CHEMBL575207 — — 1 7.52
CHEMBL209591 — — 1 7.52
CHEMBL36070 — — 1 7.40
CHEMBL209854 — — 1 7.40
CHEMBL572448 — — 1 7.40
CHEMBL572901 — — 1 7.40
CHEMBL35842 — — 1 7.30
CHEMBL209440 — — 1 7.30
CHEMBL211634 — — 1 7.16
CHEMBL212921 — — 1 7.10
CHEMBL386055 — — 1 7.05
CHEMBL516025 — — 1 7.00
CHEMBL584772 — — 1 6.89
CHEMBL573637 — — 1 6.85
CHEMBL572414 — — 1 6.82
CHEMBL572471 — — 1 6.75
CHEMBL211110 — — 1 6.72
CHEMBL573644 — — 1 6.66
CHEMBL572473 — — 1 6.60
CHEMBL214371 — — 1 6.60
CHEMBL379382 — — 1 6.48
CHEMBL564495 — — 1 6.48
CHEMBL378395 — — 1 6.46
CHEMBL492770 — — 1 6.46
CHEMBL574315 — — 1 6.34
CHEMBL573874 — — 1 6.30
CHEMBL582913 — — 1 6.30
CHEMBL573873 — — 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572902 — IC50 = 20.0 nM 7.70
CHEMBL573605 — IC50 = 20.0 nM 7.70
CHEMBL209591 — IC50 = 30.0 nM 7.52
CHEMBL575207 — IC50 = 30.0 nM 7.52
CHEMBL36070 — IC50 = 40.0 nM 7.40
CHEMBL209854 — IC50 = 40.0 nM 7.40
CHEMBL572448 — IC50 = 40.0 nM 7.40
CHEMBL572901 — IC50 = 40.0 nM 7.40
CHEMBL35842 — 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
CHEMBL386055 — IC50 = 90.0 nM 7.05
CHEMBL516025 — IC50 = 100.0 nM 7.00
CHEMBL584772 — IC50 = 130.0 nM 6.89
CHEMBL573637 — IC50 = 140.0 nM 6.85
CHEMBL572414 — IC50 = 150.0 nM 6.82
CHEMBL572471 — IC50 = 180.0 nM 6.75
CHEMBL211110 — IC50 = 190.0 nM 6.72
CHEMBL573644 — IC50 = 220.0 nM 6.66
CHEMBL572473 — IC50 = 250.0 nM 6.60
CHEMBL214371 — IC50 = 250.0 nM 6.60
CHEMBL379382 — IC50 = 330.0 nM 6.48
CHEMBL564495 — IC50 = 330.0 nM 6.48
CHEMBL378395 — IC50 = 350.0 nM 6.46
CHEMBL492770 — IC50 = 350.0 nM 6.46
CHEMBL574315 — IC50 = 460.0 nM 6.34
CHEMBL573874 — IC50 = 500.0 nM 6.30
CHEMBL582913 — IC50 = 500.0 nM 6.30
CHEMBL573873 — IC50 = 550.0 nM 6.26
CHEMBL210396 — IC50 = 760.0 nM 6.12
CHEMBL572472 — IC50 = 750.0 nM 6.12
CHEMBL377693 — IC50 = 1200.0 nM 5.92
CHEMBL211275 — IC50 = 2100.0 nM 5.68
CHEMBL574316 — IC50 = 2400.0 nM 5.62
CHEMBL212320 — IC50 = 2400.0 nM 5.62
CHEMBL564494 — IC50 = 2500.0 nM 5.60
CHEMBL583059 — IC50 = 5670.0 nM 5.25
CHEMBL573623 — IC50 = 7500.0 nM 5.12
CHEMBL573638 — IC50 = 11400.0 nM 4.94
CHEMBL573621 — IC50 < 100.0 nM -
CHEMBL584360 — IC50 < 100.0 nM -
CHEMBL572438 — IC50 < 100.0 nM -
CHEMBL242883 — IC50 < 100.0 nM -
CHEMBL574314 — IC50 < 100.0 nM -