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Assay Detail

CHEMBL650119

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

Binding
Inhibition of [125I]RANTES binding to CCR5 receptor.
23
Total Activities
23
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

Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.
Palani A, Shapiro S, Clader JW, Greenlee WJ, Vice S, McCombie S, Cox K, Strizki J, Baroudy BM.
Bioorg Med Chem Lett (2003) 13 : 709 -712
PubMed 12639564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.29 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL349008 1 9.52
CHEMBL350563 1 9.40
CHEMBL162880 1 9.15
CHEMBL164484 1 8.92
CHEMBL140418 1 8.89
CHEMBL140390 1 8.70
CHEMBL82301 VICRIVIROC 3.0 1 8.68
CHEMBL335120 1 8.68
CHEMBL351625 1 8.66
CHEMBL140552 1 8.49
CHEMBL140912 1 8.48
CHEMBL161587 1 8.33
CHEMBL343520 1 8.28
CHEMBL141683 1 8.24
CHEMBL341758 1 8.09
CHEMBL161664 1 8.06
CHEMBL344435 1 7.96
CHEMBL141201 1 7.85
CHEMBL162946 1 7.64
CHEMBL139246 1 7.60
CHEMBL139701 1 7.37
CHEMBL140201 1 7.22
CHEMBL342706 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL349008 Ki = 0.3 nM 9.52
CHEMBL350563 Ki = 0.4 nM 9.40
CHEMBL162880 Ki = 0.7 nM 9.15
CHEMBL164484 Ki = 1.2 nM 8.92
CHEMBL140418 Ki = 1.3 nM 8.89
CHEMBL140390 Ki = 2.0 nM 8.70
CHEMBL82301 VICRIVIROC Ki = 2.1 nM 8.68
CHEMBL335120 Ki = 2.1 nM 8.68
CHEMBL351625 Ki = 2.2 nM 8.66
CHEMBL140552 Ki = 3.2 nM 8.49
CHEMBL140912 Ki = 3.3 nM 8.48
CHEMBL161587 Ki = 4.7 nM 8.33
CHEMBL343520 Ki = 5.3 nM 8.28
CHEMBL141683 Ki = 5.7 nM 8.24
CHEMBL341758 Ki = 8.1 nM 8.09
CHEMBL161664 Ki = 8.8 nM 8.06
CHEMBL344435 Ki = 11.0 nM 7.96
CHEMBL141201 Ki = 14.0 nM 7.85
CHEMBL162946 Ki = 23.0 nM 7.64
CHEMBL139246 Ki = 25.0 nM 7.60
CHEMBL139701 Ki = 43.0 nM 7.37
CHEMBL140201 Ki = 60.0 nM 7.22
CHEMBL342706 Ki = 315.0 nM 6.50