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Assay Detail

CHEMBL616207

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

Binding
In vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of a new model of arylpiperazines. Study of the 5-HT(1a)/alpha(1)-adrenergic receptor affinity by classical hansch analysis, artificial neural networks, and computational simulation of ligand recognition.
López-Rodríguez ML, Morcillo MJ, Fernández E, Rosado ML, Pardo L, Schaper K.
J Med Chem (2001) 44 : 198 -207
PubMed 11170629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.32 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294074 1 9.22
CHEMBL61545 1 8.66
CHEMBL62694 1 8.47
CHEMBL61614 1 8.40
CHEMBL62017 1 8.32
CHEMBL59791 1 8.27
CHEMBL61250 1 8.26
CHEMBL292315 1 8.06
CHEMBL292279 1 7.92
CHEMBL58006 1 7.82
CHEMBL60973 1 7.82
CHEMBL417381 1 7.80
CHEMBL58850 1 7.57
CHEMBL416266 1 7.57
CHEMBL59282 1 7.55
CHEMBL58702 1 7.50
CHEMBL61473 1 7.47
CHEMBL58197 1 7.34
CHEMBL59778 1 7.32
CHEMBL60078 1 7.26
CHEMBL57953 1 7.19
CHEMBL293365 1 7.17
CHEMBL293488 1 7.04
CHEMBL301637 1 6.84
CHEMBL294837 1 6.75
CHEMBL1202594 1 6.71
CHEMBL61904 1 6.70
CHEMBL417213 1 6.66
CHEMBL58946 1 6.58
CHEMBL59892 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294074 Ki = 0.6 nM 9.22
CHEMBL61545 Ki = 2.2 nM 8.66
CHEMBL62694 Ki = 3.4 nM 8.47
CHEMBL61614 Ki = 4.0 nM 8.40
CHEMBL62017 Ki = 4.8 nM 8.32
CHEMBL59791 Ki = 5.4 nM 8.27
CHEMBL61250 Ki = 5.5 nM 8.26
CHEMBL292315 Ki = 8.7 nM 8.06
CHEMBL292279 Ki = 12.0 nM 7.92
CHEMBL58006 Ki = 15.0 nM 7.82
CHEMBL60973 Ki = 15.0 nM 7.82
CHEMBL417381 Ki = 16.0 nM 7.80
CHEMBL58850 Ki = 27.0 nM 7.57
CHEMBL416266 Ki = 27.0 nM 7.57
CHEMBL59282 Ki = 28.0 nM 7.55
CHEMBL58702 Ki = 32.0 nM 7.50
CHEMBL61473 Ki = 34.0 nM 7.47
CHEMBL58197 Ki = 46.0 nM 7.34
CHEMBL59778 Ki = 48.0 nM 7.32
CHEMBL60078 Ki = 55.0 nM 7.26
CHEMBL57953 Ki = 65.0 nM 7.19
CHEMBL293365 Ki = 68.0 nM 7.17
CHEMBL293488 Ki = 92.0 nM 7.04
CHEMBL301637 Ki = 143.0 nM 6.84
CHEMBL294837 Ki = 179.0 nM 6.75
CHEMBL1202594 Ki = 193.0 nM 6.71
CHEMBL61904 Ki = 198.0 nM 6.70
CHEMBL417213 Ki = 220.0 nM 6.66
CHEMBL58946 Ki = 266.0 nM 6.58
CHEMBL59892 Ki = 378.0 nM 6.42
CHEMBL59062 Ki = 776.0 nM 6.11
CHEMBL418638 Ki = 808.0 nM 6.09
CHEMBL59950 Ki = 1182.0 nM 5.93
CHEMBL293048 Ki = 1232.0 nM 5.91
CHEMBL60211 Ki = 4614.0 nM 5.34