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Assay Detail

CHEMBL616057

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampal membranes
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
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 7.15 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286725 1 10.22
CHEMBL152756 1 9.37
CHEMBL345848 1 9.22
CHEMBL56 8-OH-DPAT 1 8.68
CHEMBL152869 1 8.35
CHEMBL152159 1 8.12
CHEMBL152587 1 7.90
CHEMBL357448 1 7.70
CHEMBL157322 1 7.57
CHEMBL147483 1 7.57
CHEMBL156599 1 7.54
CHEMBL157388 1 7.46
CHEMBL2112905 1 7.23
CHEMBL157222 1 7.23
CHEMBL347290 1 7.10
CHEMBL152304 1 7.05
CHEMBL152576 1 6.93
CHEMBL152391 1 6.91
CHEMBL2112911 1 6.90
CHEMBL93403 1 6.83
CHEMBL196476 1 6.74
CHEMBL433741 1 6.57
CHEMBL154050 1 6.50
CHEMBL154508 1 6.47
CHEMBL315879 1 6.40
CHEMBL156845 1 6.37
CHEMBL345111 1 6.36
CHEMBL345820 1 6.24
CHEMBL152010 1 6.21
CHEMBL152262 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286725 Ki = 0.06 nM 10.22
CHEMBL152756 Ki = 0.43 nM 9.37
CHEMBL345848 Ki = 0.6 nM 9.22
CHEMBL56 8-OH-DPAT Ki = 2.1 nM 8.68
CHEMBL152869 Ki = 4.5 nM 8.35
CHEMBL152159 Ki = 7.5 nM 8.12
CHEMBL152587 Ki = 12.7 nM 7.90
CHEMBL357448 Ki = 19.8 nM 7.70
CHEMBL157322 Ki = 27.0 nM 7.57
CHEMBL147483 Ki = 27.0 nM 7.57
CHEMBL156599 Ki = 29.0 nM 7.54
CHEMBL157388 Ki = 35.0 nM 7.46
CHEMBL2112905 Ki = 58.6 nM 7.23
CHEMBL157222 Ki = 59.0 nM 7.23
CHEMBL347290 Ki = 78.7 nM 7.10
CHEMBL152304 Ki = 88.5 nM 7.05
CHEMBL152576 Ki = 117.0 nM 6.93
CHEMBL152391 Ki = 123.0 nM 6.91
CHEMBL2112911 Ki = 126.0 nM 6.90
CHEMBL93403 Ki = 147.0 nM 6.83
CHEMBL196476 Ki = 184.0 nM 6.74
CHEMBL433741 Ki = 268.0 nM 6.57
CHEMBL154050 Ki = 313.0 nM 6.50
CHEMBL154508 Ki = 335.0 nM 6.47
CHEMBL315879 Ki = 397.0 nM 6.40
CHEMBL156845 Ki = 432.0 nM 6.37
CHEMBL345111 Ki = 433.0 nM 6.36
CHEMBL345820 Ki = 575.0 nM 6.24
CHEMBL152010 Ki = 621.0 nM 6.21
CHEMBL152262 Ki = 1110.0 nM 5.96
CHEMBL346692 Ki = 1660.0 nM 5.78
CHEMBL2112910 Ki = 5500.0 nM 5.26
CHEMBL423040 Ki = 7730.0 nM 5.11
CHEMBL152679 Ki > 850.0 nM -
CHEMBL305362 Ki > 1000.0 nM -
CHEMBL92713 Ki > 850.0 nM -
CHEMBL61789 Ki > 1000.0 nM -
CHEMBL94265 Ki > 850.0 nM -