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Assay Detail

CHEMBL643852

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

Functional
Antagonistic activity upon postsynaptic alpha-1 adrenergic receptor was determined in the rat isolated, field stimulated vas deferens using methoxamine
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
Saari WS, Halczenko W, Huff JR, Guare JP, Hunt CA, Randall WC, Lotti VJ, Yarbrough GG.
J Med Chem (1984) 27 : 1182 -1185
PubMed 6088770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.05 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6437 MIANSERIN 4.0 1 7.24
CHEMBL15245 YOHIMBINE 3.0 1 6.52
CHEMBL280514 1 6.20
CHEMBL10347 RAUWOLSCINE 1 6.00
CHEMBL18094 1 5.70
CHEMBL17605 1 5.40
CHEMBL18194 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6437 MIANSERIN Kd = 57.54 nM 7.24
CHEMBL15245 YOHIMBINE Kd = 302.0 nM 6.52
CHEMBL280514 Kd = 630.96 nM 6.20
CHEMBL10347 RAUWOLSCINE Kd = 1000.0 nM 6.00
CHEMBL18094 Kd = 1995.26 nM 5.70
CHEMBL17605 Kd = 3981.07 nM 5.40
CHEMBL18194 Kd = 5011.87 nM 5.30