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Assay Detail

CHEMBL661605

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Binding
Inhibition of [125I]-MIP-1 alpha binding to human CCR5 receptor expressed in Chinese hamster ovary (CHO) cells
ChEMBL ↗
55
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
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 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
Finke PE, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, 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 : 2475 -2479
PubMed 11549450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 55 7.93 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432360 — — 1 9.12
CHEMBL310106 — — 1 9.10
CHEMBL82168 — — 1 8.82
CHEMBL2114183 — — 1 8.82
CHEMBL421342 — — 1 8.82
CHEMBL82048 — — 1 8.70
CHEMBL79622 — — 1 8.70
CHEMBL311549 — — 1 8.70
CHEMBL311248 — — 1 8.70
CHEMBL85086 — — 1 8.70
CHEMBL2114184 — — 1 8.70
CHEMBL83335 — — 1 8.70
CHEMBL81252 — — 1 8.70
CHEMBL79530 — — 1 8.60
CHEMBL81245 — — 1 8.52
CHEMBL83823 — — 1 8.52
CHEMBL83057 — — 1 8.52
CHEMBL311261 — — 1 8.52
CHEMBL84309 — — 1 8.40
CHEMBL81926 — — 1 8.40
CHEMBL445836 — — 1 8.40
CHEMBL313216 — — 1 8.40
CHEMBL432182 — — 1 8.30
CHEMBL309619 — — 1 8.30
CHEMBL82880 — — 1 8.30
CHEMBL79770 — — 1 8.22
CHEMBL80043 — — 1 8.22
CHEMBL311052 — — 1 8.22
CHEMBL79667 — — 1 8.00
CHEMBL311532 — — 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432360 — IC50 = 0.75 nM 9.12
CHEMBL310106 — IC50 = 0.8 nM 9.10
CHEMBL82168 — IC50 = 1.5 nM 8.82
CHEMBL2114183 — IC50 = 1.5 nM 8.82
CHEMBL421342 — IC50 = 1.5 nM 8.82
CHEMBL82048 — IC50 = 2.0 nM 8.70
CHEMBL79622 — IC50 = 2.0 nM 8.70
CHEMBL311549 — IC50 = 2.0 nM 8.70
CHEMBL311248 — IC50 = 2.0 nM 8.70
CHEMBL85086 — IC50 = 2.0 nM 8.70
CHEMBL2114184 — IC50 = 2.0 nM 8.70
CHEMBL83335 — IC50 = 2.0 nM 8.70
CHEMBL81252 — IC50 = 2.0 nM 8.70
CHEMBL79530 — IC50 = 2.5 nM 8.60
CHEMBL311261 — IC50 = 3.0 nM 8.52
CHEMBL81245 — IC50 = 3.0 nM 8.52
CHEMBL83057 — IC50 = 3.0 nM 8.52
CHEMBL83823 — IC50 = 3.0 nM 8.52
CHEMBL84309 — IC50 = 4.0 nM 8.40
CHEMBL81926 — IC50 = 4.0 nM 8.40
CHEMBL445836 — IC50 = 4.0 nM 8.40
CHEMBL313216 — IC50 = 4.0 nM 8.40
CHEMBL432182 — IC50 = 5.0 nM 8.30
CHEMBL309619 — IC50 = 5.0 nM 8.30
CHEMBL82880 — IC50 = 5.0 nM 8.30
CHEMBL79770 — IC50 = 6.0 nM 8.22
CHEMBL311052 — IC50 = 6.0 nM 8.22
CHEMBL80043 — IC50 = 6.0 nM 8.22
CHEMBL79667 — IC50 = 10.0 nM 8.00
CHEMBL311532 — IC50 = 10.0 nM 8.00
CHEMBL83338 — IC50 = 10.0 nM 8.00
CHEMBL309657 — IC50 = 15.0 nM 7.82
CHEMBL431009 — IC50 = 15.0 nM 7.82
CHEMBL79907 — IC50 = 20.0 nM 7.70
CHEMBL309447 — IC50 = 20.0 nM 7.70
CHEMBL82786 — IC50 = 20.0 nM 7.70
CHEMBL79930 — IC50 = 25.0 nM 7.60
CHEMBL79930 — IC50 = 30.0 nM 7.52
CHEMBL79504 — IC50 = 35.0 nM 7.46
CHEMBL312945 — IC50 = 35.0 nM 7.46
CHEMBL81719 — IC50 = 35.0 nM 7.46
CHEMBL310645 — IC50 = 40.0 nM 7.40
CHEMBL84029 — IC50 = 40.0 nM 7.40
CHEMBL83113 — IC50 = 75.0 nM 7.12
CHEMBL309922 — IC50 = 100.0 nM 7.00
CHEMBL82879 — IC50 = 100.0 nM 7.00
CHEMBL79315 — IC50 = 100.0 nM 7.00
CHEMBL430818 — IC50 = 120.0 nM 6.92
CHEMBL84268 — IC50 = 120.0 nM 6.92
CHEMBL440137 — IC50 = 150.0 nM 6.82