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Assay Detail

CHEMBL641369

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

Functional
Antagonistic activity against clonidine-stimulated rat vas deferens presynaptic alpha-2 adrenergic receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
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 13 7.09 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10347 RAUWOLSCINE 1 7.90
CHEMBL15245 YOHIMBINE 3.0 1 7.65
CHEMBL280514 1 7.40
CHEMBL6437 MIANSERIN 4.0 1 7.27
CHEMBL18194 1 6.80
CHEMBL18094 1 6.40
CHEMBL17605 1 6.20
CHEMBL18306 1 -
CHEMBL17223 1 -
CHEMBL17648 1 -
CHEMBL17926 1 -
CHEMBL18270 1 -
CHEMBL278934 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10347 RAUWOLSCINE Kd = 12.59 nM 7.90
CHEMBL15245 YOHIMBINE Kd = 22.39 nM 7.65
CHEMBL280514 Kd = 39.81 nM 7.40
CHEMBL6437 MIANSERIN Kd = 53.7 nM 7.27
CHEMBL18194 Kd = 158.49 nM 6.80
CHEMBL18094 Kd = 398.11 nM 6.40
CHEMBL17605 Kd = 630.96 nM 6.20
CHEMBL18306 Kd > 1584.89 nM -
CHEMBL17223 Kd > 1584.89 nM -
CHEMBL17648 Kd > 1584.89 nM -
CHEMBL17926 Kd > 1258.93 nM -
CHEMBL18270 Kd > 1584.89 nM -
CHEMBL278934 Kd > 1995.26 nM -