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Assay Detail

CHEMBL646866

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

Binding
Binding affinity was tested on Alpha-1 adrenergic receptor using radioligand [3H](+)-pentazocine binding assay.
16
Total Activities
16
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

Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives.
Berardi F, Giudice G, Perrone R, Tortorella V, Govoni S, Lucchi L.
J Med Chem (1996) 39 : 4255 -4260
PubMed 8863803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.22 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127006 1 9.40
CHEMBL128442 1 9.10
CHEMBL337709 1 8.43
CHEMBL435397 1 8.41
CHEMBL423349 1 8.41
CHEMBL134717 1 8.41
CHEMBL135530 1 8.41
CHEMBL135528 1 8.33
CHEMBL334440 1 8.33
CHEMBL135930 1 8.17
CHEMBL54 HALOPERIDOL 4.0 1 8.00
CHEMBL134607 1 7.74
CHEMBL336378 1 7.52
CHEMBL134504 1 7.40
CHEMBL135738 1 7.20
CHEMBL135687 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127006 Ki = 0.4 nM 9.40
CHEMBL128442 Ki = 0.8 nM 9.10
CHEMBL337709 Ki = 3.7 nM 8.43
CHEMBL435397 Ki = 3.9 nM 8.41
CHEMBL423349 Ki = 3.9 nM 8.41
CHEMBL134717 Ki = 3.9 nM 8.41
CHEMBL135530 Ki = 3.9 nM 8.41
CHEMBL135528 Ki = 4.7 nM 8.33
CHEMBL334440 Ki = 4.7 nM 8.33
CHEMBL135930 Ki = 6.7 nM 8.17
CHEMBL54 HALOPERIDOL Ki = 10.0 nM 8.00
CHEMBL134607 Ki = 18.2 nM 7.74
CHEMBL336378 Ki = 30.0 nM 7.52
CHEMBL134504 Ki = 40.0 nM 7.40
CHEMBL135738 Ki = 63.2 nM 7.20
CHEMBL135687 Ki > 3960.0 nM -