Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL839696

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

Binding
Inhibitory constant was determined against 5-hydroxytryptamine 1A receptor using 1.2 nM [3H]8-OH-DPAT
29
Total Activities
29
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

Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
Costantino L, Gandolfi F, Sorbi C, Franchini S, Prezzavento O, Vittorio F, Ronsisvalle G, Leonardi A, Poggesi E, Brasili L.
J Med Chem (2005) 48 : 266 -273
PubMed 15634021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.16 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL537403 1 9.22
CHEMBL178650 1 7.94
CHEMBL178700 1 7.75
CHEMBL179648 1 7.68
CHEMBL178680 1 7.27
CHEMBL179371 1 7.24
CHEMBL359663 1 7.16
CHEMBL426958 1 6.92
CHEMBL180327 1 6.76
CHEMBL369091 1 6.73
CHEMBL179373 1 6.65
CHEMBL178519 1 6.58
CHEMBL434905 1 6.58
CHEMBL179397 1 6.53
CHEMBL425867 1 6.35
CHEMBL180180 1 -
CHEMBL369133 1 -
CHEMBL179808 1 -
CHEMBL179145 1 -
CHEMBL276784 1 -
CHEMBL179651 1 -
CHEMBL178988 1 -
CHEMBL179530 1 -
CHEMBL179062 1 -
CHEMBL360351 1 -
CHEMBL362699 1 -
CHEMBL178924 1 -
CHEMBL179697 1 -
CHEMBL180119 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL537403 Ki = 0.6 nM 9.22
CHEMBL178650 Ki = 11.5 nM 7.94
CHEMBL178700 Ki = 17.6 nM 7.75
CHEMBL179648 Ki = 20.7 nM 7.68
CHEMBL178680 Ki = 54.2 nM 7.27
CHEMBL179371 Ki = 57.2 nM 7.24
CHEMBL359663 Ki = 69.4 nM 7.16
CHEMBL426958 Ki = 120.0 nM 6.92
CHEMBL180327 Ki = 172.0 nM 6.76
CHEMBL369091 Ki = 185.0 nM 6.73
CHEMBL179373 Ki = 226.0 nM 6.65
CHEMBL178519 Ki = 260.0 nM 6.58
CHEMBL434905 Ki = 260.0 nM 6.58
CHEMBL179397 Ki = 297.0 nM 6.53
CHEMBL425867 Ki = 445.0 nM 6.35
CHEMBL180180 Ki > 1000.0 nM -
CHEMBL369133 Ki > 1000.0 nM -
CHEMBL179808 Ki > 1000.0 nM -
CHEMBL179145 Ki > 1000.0 nM -
CHEMBL276784 Ki > 1000.0 nM -
CHEMBL179651 Ki > 1000.0 nM -
CHEMBL178988 Ki > 1000.0 nM -
CHEMBL179530 Ki > 1000.0 nM -
CHEMBL179062 Ki > 1000.0 nM -
CHEMBL360351 Ki > 1000.0 nM -
CHEMBL362699 Ki > 1000.0 nM -
CHEMBL178924 Ki > 1000.0 nM -
CHEMBL179697 Ki > 1000.0 nM -
CHEMBL180119 Ki > 1000.0 nM -