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Assay Detail

CHEMBL641538

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

Functional
Antagonistic activity against presynaptic alpha-2 adrenergic receptor in isolated rat vas deferens using xylazine as agonist
23
Total Activities
23
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-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
Vizi ES, Toth I, Somogyi GT, Szabo L, Harsing LG, Szantay C.
J Med Chem (1987) 30 : 1355 -1359
PubMed 2886664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 23 6.78 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28531 1 8.17
CHEMBL10316 IDAZOXAN 3.0 1 8.07
CHEMBL597 PHENTOLAMINE 4.0 1 7.78
CHEMBL15245 YOHIMBINE 3.0 1 7.72
CHEMBL29379 1 7.63
CHEMBL282636 1 7.41
CHEMBL25979 1 7.39
CHEMBL29869 1 7.30
CHEMBL281708 1 7.18
CHEMBL26156 1 7.12
CHEMBL2 PRAZOSIN 4.0 1 6.84
CHEMBL280650 1 6.77
CHEMBL280810 1 6.61
CHEMBL424034 1 6.41
CHEMBL416757 1 6.31
CHEMBL27522 1 6.21
CHEMBL283875 1 6.21
CHEMBL286033 1 6.10
CHEMBL30114 1 5.91
CHEMBL25982 1 5.80
CHEMBL27355 1 5.74
CHEMBL26421 1 5.64
CHEMBL29380 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28531 Kd = 6.761 nM 8.17
CHEMBL10316 IDAZOXAN Kd = 8.511 nM 8.07
CHEMBL597 PHENTOLAMINE Kd = 16.6 nM 7.78
CHEMBL15245 YOHIMBINE Kd = 19.05 nM 7.72
CHEMBL29379 Kd = 23.44 nM 7.63
CHEMBL282636 Kd = 38.9 nM 7.41
CHEMBL25979 Kd = 40.74 nM 7.39
CHEMBL29869 Kd = 50.12 nM 7.30
CHEMBL281708 Kd = 66.07 nM 7.18
CHEMBL26156 Kd = 75.86 nM 7.12
CHEMBL2 PRAZOSIN Kd = 144.54 nM 6.84
CHEMBL280650 Kd = 169.82 nM 6.77
CHEMBL280810 Kd = 245.47 nM 6.61
CHEMBL424034 Kd = 389.05 nM 6.41
CHEMBL416757 Kd = 489.78 nM 6.31
CHEMBL27522 Kd = 616.6 nM 6.21
CHEMBL283875 Kd = 616.6 nM 6.21
CHEMBL286033 Kd = 794.33 nM 6.10
CHEMBL30114 Kd = 1230.27 nM 5.91
CHEMBL25982 Kd = 1584.89 nM 5.80
CHEMBL27355 Kd = 1819.7 nM 5.74
CHEMBL26421 Kd = 2290.87 nM 5.64
CHEMBL29380 Kd = 2511.89 nM 5.60