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Assay Detail

CHEMBL661607

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Binding
Inhibitory activity against specific binding of [125I]-MIP-1 alpha to human CCR5 receptor.
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

C-C chemokine receptor type 5 (CHEMBL274) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Finke PE, Meurer LC, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA.
Bioorg Med Chem Lett (2001) 11 : 265 -270
PubMed 11206474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.76 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83338 — — 1 8.00
CHEMBL83107 — — 1 7.82
CHEMBL89958 — — 1 7.52
CHEMBL312701 — — 1 7.52
CHEMBL408438 — — 1 7.46
CHEMBL79504 — — 1 7.46
CHEMBL418954 — — 1 7.30
CHEMBL316189 — — 1 7.22
CHEMBL328898 — — 1 7.10
CHEMBL88197 — — 1 7.10
CHEMBL92147 — — 1 7.05
CHEMBL421356 — — 1 7.00
CHEMBL90747 — — 1 7.00
CHEMBL89715 — — 1 7.00
CHEMBL91522 — — 1 7.00
CHEMBL90141 — — 1 6.96
CHEMBL91374 — — 1 6.96
CHEMBL328908 — — 1 6.96
CHEMBL88164 — — 1 6.96
CHEMBL327484 — — 1 6.92
CHEMBL91892 — — 1 6.80
CHEMBL88219 — — 1 6.75
CHEMBL90291 — — 1 6.75
CHEMBL92094 — — 1 6.70
CHEMBL328339 — — 1 6.70
CHEMBL432040 — — 1 6.57
CHEMBL79716 — — 1 6.57
CHEMBL330486 — — 1 6.52
CHEMBL90691 — — 1 6.52
CHEMBL328888 — — 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83338 — IC50 = 10.0 nM 8.00
CHEMBL83107 — IC50 = 15.0 nM 7.82
CHEMBL312701 — IC50 = 30.0 nM 7.52
CHEMBL89958 — IC50 = 30.0 nM 7.52
CHEMBL408438 — IC50 = 35.0 nM 7.46
CHEMBL79504 — IC50 = 35.0 nM 7.46
CHEMBL418954 — IC50 = 50.0 nM 7.30
CHEMBL316189 — IC50 = 60.0 nM 7.22
CHEMBL328898 — IC50 = 80.0 nM 7.10
CHEMBL88197 — IC50 = 80.0 nM 7.10
CHEMBL92147 — IC50 = 90.0 nM 7.05
CHEMBL91522 — IC50 = 100.0 nM 7.00
CHEMBL89715 — IC50 = 100.0 nM 7.00
CHEMBL90747 — IC50 = 100.0 nM 7.00
CHEMBL421356 — IC50 = 100.0 nM 7.00
CHEMBL90141 — IC50 = 110.0 nM 6.96
CHEMBL88164 — IC50 = 110.0 nM 6.96
CHEMBL328908 — IC50 = 110.0 nM 6.96
CHEMBL91374 — IC50 = 110.0 nM 6.96
CHEMBL327484 — IC50 = 120.0 nM 6.92
CHEMBL91892 — IC50 = 160.0 nM 6.80
CHEMBL88219 — IC50 = 180.0 nM 6.75
CHEMBL90291 — IC50 = 180.0 nM 6.75
CHEMBL92094 — IC50 = 200.0 nM 6.70
CHEMBL328339 — IC50 = 200.0 nM 6.70
CHEMBL432040 — IC50 = 270.0 nM 6.57
CHEMBL79716 — IC50 = 270.0 nM 6.57
CHEMBL330486 — IC50 = 300.0 nM 6.52
CHEMBL90691 — IC50 = 300.0 nM 6.52
CHEMBL328888 — IC50 = 400.0 nM 6.40
CHEMBL88455 — IC50 = 450.0 nM 6.35
CHEMBL91413 — IC50 = 500.0 nM 6.30
CHEMBL88927 — IC50 = 570.0 nM 6.24
CHEMBL313950 — IC50 = 570.0 nM 6.24
CHEMBL329190 — IC50 = 720.0 nM 6.14
CHEMBL420057 — IC50 = 1000.0 nM 6.00
CHEMBL328438 — IC50 = 1300.0 nM 5.89
CHEMBL89929 — IC50 = 2000.0 nM 5.70
CHEMBL420242 — IC50 = 3000.0 nM 5.52
CHEMBL327880 — IC50 = 4000.0 nM 5.40
CHEMBL316280 — IC50 > 1000.0 nM -
CHEMBL89490 — IC50 ~ 10000.0 nM -
CHEMBL91387 — IC50 ~ 1000.0 nM -
CHEMBL328088 — IC50 > 1000.0 nM -
CHEMBL90152 — IC50 > 1000.0 nM -
CHEMBL88928 — IC50 > 1000.0 nM -
CHEMBL330252 — IC50 ~ 10000.0 nM -
CHEMBL90841 — IC50 > 10000.0 nM -
CHEMBL92791 — IC50 > 1000.0 nM -
CHEMBL90927 — IC50 ~ 10000.0 nM -