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Assay Detail

CHEMBL647023

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor from rat cortical membranes
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
Leopoldo M, Berardi F, Colabufo NA, De Giorgio P, Lacivita E, Perrone R, Tortorella V.
J Med Chem (2002) 45 : 5727 -5735
PubMed 12477356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 6.65 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL154508 1 8.30
CHEMBL345848 1 8.14
CHEMBL152869 1 7.79
CHEMBL597 PHENTOLAMINE 4.0 1 7.75
CHEMBL157322 1 7.75
CHEMBL152159 1 7.58
CHEMBL152756 1 7.24
CHEMBL357448 1 7.21
CHEMBL152576 1 7.18
CHEMBL347290 1 7.04
CHEMBL196476 1 6.96
CHEMBL345111 1 6.94
CHEMBL154050 1 6.87
CHEMBL152391 1 6.87
CHEMBL152304 1 6.86
CHEMBL286725 1 6.75
CHEMBL157222 1 6.71
CHEMBL157388 1 6.65
CHEMBL2112911 1 6.63
CHEMBL93403 1 6.61
CHEMBL147483 1 6.55
CHEMBL315879 1 6.39
CHEMBL156599 1 6.37
CHEMBL92713 1 6.36
CHEMBL156845 1 6.34
CHEMBL94265 1 6.33
CHEMBL2112910 1 6.18
CHEMBL433741 1 6.14
CHEMBL152587 1 5.95
CHEMBL152010 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL154508 Ki = 5.0 nM 8.30
CHEMBL345848 Ki = 7.3 nM 8.14
CHEMBL152869 Ki = 16.2 nM 7.79
CHEMBL597 PHENTOLAMINE Ki = 18.0 nM 7.75
CHEMBL157322 Ki = 18.0 nM 7.75
CHEMBL152159 Ki = 26.4 nM 7.58
CHEMBL152756 Ki = 57.0 nM 7.24
CHEMBL357448 Ki = 61.4 nM 7.21
CHEMBL152576 Ki = 66.7 nM 7.18
CHEMBL347290 Ki = 92.1 nM 7.04
CHEMBL196476 Ki = 110.0 nM 6.96
CHEMBL345111 Ki = 115.0 nM 6.94
CHEMBL154050 Ki = 134.0 nM 6.87
CHEMBL152391 Ki = 134.0 nM 6.87
CHEMBL152304 Ki = 138.0 nM 6.86
CHEMBL286725 Ki = 180.0 nM 6.75
CHEMBL157222 Ki = 197.0 nM 6.71
CHEMBL157388 Ki = 224.0 nM 6.65
CHEMBL2112911 Ki = 236.0 nM 6.63
CHEMBL93403 Ki = 245.0 nM 6.61
CHEMBL147483 Ki = 283.0 nM 6.55
CHEMBL315879 Ki = 406.0 nM 6.39
CHEMBL156599 Ki = 425.0 nM 6.37
CHEMBL92713 Ki = 437.0 nM 6.36
CHEMBL156845 Ki = 454.0 nM 6.34
CHEMBL94265 Ki = 470.0 nM 6.33
CHEMBL2112910 Ki = 656.0 nM 6.18
CHEMBL433741 Ki = 717.0 nM 6.14
CHEMBL152010 Ki = 1120.0 nM 5.95
CHEMBL152587 Ki = 1120.0 nM 5.95
CHEMBL152262 Ki = 1880.0 nM 5.73
CHEMBL346692 Ki = 2050.0 nM 5.69
CHEMBL2112905 Ki = 2900.0 nM 5.54
CHEMBL423040 Ki = 3119.0 nM 5.51
CHEMBL345820 Ki = 5100.0 nM 5.29
CHEMBL152679 Ki = 5900.0 nM 5.23
CHEMBL61789 Ki > 1000.0 nM -
CHEMBL305362 Ki > 1000.0 nM -