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Assay Detail

CHEMBL616136

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

Binding
Affinity for 5-hydroxytryptamine 1A receptor subtype
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B receptor antagonists
Jorand-Lebrun C, Pauwels P, Palmier C, Chopin P, Moret C, Marien M, Halazy S
Bioorg Med Chem Lett (1997) 7 : 3183 -3188
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.55 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321818 1 8.10
CHEMBL15928 GR-127935 1 7.14
CHEMBL108722 1 7.10
CHEMBL325359 1 6.59
CHEMBL111302 1 6.41
CHEMBL105970 1 6.41
CHEMBL325131 1 6.35
CHEMBL323986 1 6.24
CHEMBL430500 1 6.16
CHEMBL108645 1 6.00
CHEMBL110601 1 5.52
CHEMBL107772 1 -
CHEMBL106807 1 -
CHEMBL281350 SB-224289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321818 Ki = 8.0 nM 8.10
CHEMBL15928 GR-127935 Ki = 72.0 nM 7.14
CHEMBL108722 Ki = 79.0 nM 7.10
CHEMBL325359 Ki = 257.0 nM 6.59
CHEMBL111302 Ki = 393.0 nM 6.41
CHEMBL105970 Ki = 390.0 nM 6.41
CHEMBL325131 Ki = 450.0 nM 6.35
CHEMBL323986 Ki = 571.0 nM 6.24
CHEMBL430500 Ki = 700.0 nM 6.16
CHEMBL108645 Ki = 1000.0 nM 6.00
CHEMBL110601 Ki = 3000.0 nM 5.52
CHEMBL107772 Ki > 1000.0 nM -
CHEMBL106807 Ki > 1000.0 nM -
CHEMBL281350 SB-224289 Ki > 1000.0 nM -