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Assay Detail

CHEMBL641537

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

Functional
Antagonistic activity against alpha-2 adrenergic receptor in rat vas deferens
51
Total Activities
48
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

Synthesis and structure-activity relationships of 2-sulfonamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines as alpha 2-adrenoceptor antagonists.
Ward TJ, White JF, Lattimer N, Rhodes KF, Sharma S, Waterfall JF.
J Med Chem (1988) 31 : 1421 -1426
PubMed 2838634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 51 7.50 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30419 2 8.50
CHEMBL30979 1 8.46
CHEMBL277737 1 8.44
CHEMBL280750 1 8.26
CHEMBL33498 1 8.22
CHEMBL30477 2 8.16
CHEMBL33443 1 8.11
CHEMBL283498 1 8.10
CHEMBL30829 1 8.10
CHEMBL285807 1 8.10
CHEMBL30651 1 8.06
CHEMBL442104 2 8.05
CHEMBL10316 IDAZOXAN 3.0 1 8.04
CHEMBL285992 1 7.94
CHEMBL33231 1 7.93
CHEMBL34330 1 7.90
CHEMBL287245 1 7.87
CHEMBL281107 1 7.87
CHEMBL34570 1 7.77
CHEMBL30338 1 7.74
CHEMBL282848 1 7.70
CHEMBL30462 1 7.70
CHEMBL30956 1 7.61
CHEMBL282182 1 7.60
CHEMBL15245 YOHIMBINE 3.0 1 7.58
CHEMBL30504 1 7.56
CHEMBL417484 1 7.50
CHEMBL286650 1 7.44
CHEMBL282098 1 7.40
CHEMBL30590 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30419 Kd = 3.162 nM 8.50
CHEMBL30979 Kd = 3.467 nM 8.46
CHEMBL277737 Kd = 3.631 nM 8.44
CHEMBL280750 Kd = 5.495 nM 8.26
CHEMBL33498 Kd = 6.026 nM 8.22
CHEMBL30477 Kd = 6.918 nM 8.16
CHEMBL33443 Kd = 7.762 nM 8.11
CHEMBL283498 Kd = 7.943 nM 8.10
CHEMBL285807 Kd = 7.943 nM 8.10
CHEMBL30829 Kd = 7.943 nM 8.10
CHEMBL30419 Kd = 8.318 nM 8.08
CHEMBL30651 Kd = 8.71 nM 8.06
CHEMBL30477 Kd = 8.913 nM 8.05
CHEMBL442104 Kd = 8.913 nM 8.05
CHEMBL10316 IDAZOXAN Kd = 9.12 nM 8.04
CHEMBL285992 Kd = 11.48 nM 7.94
CHEMBL33231 Kd = 11.75 nM 7.93
CHEMBL34330 Kd = 12.59 nM 7.90
CHEMBL287245 Kd = 13.49 nM 7.87
CHEMBL281107 Kd = 13.49 nM 7.87
CHEMBL442104 Kd = 15.49 nM 7.81
CHEMBL34570 Kd = 16.98 nM 7.77
CHEMBL30338 Kd = 18.2 nM 7.74
CHEMBL282848 Kd = 19.95 nM 7.70
CHEMBL30462 Kd = 19.95 nM 7.70
CHEMBL30956 Kd = 24.55 nM 7.61
CHEMBL282182 Kd = 25.12 nM 7.60
CHEMBL15245 YOHIMBINE Kd = 26.3 nM 7.58
CHEMBL30504 Kd = 27.54 nM 7.56
CHEMBL417484 Kd = 31.62 nM 7.50
CHEMBL286650 Kd = 36.31 nM 7.44
CHEMBL282098 Kd = 39.81 nM 7.40
CHEMBL30590 Kd = 40.74 nM 7.39
CHEMBL416403 Kd = 54.95 nM 7.26
CHEMBL31045 Kd = 70.79 nM 7.15
CHEMBL30704 Kd = 79.43 nM 7.10
CHEMBL287294 Kd = 79.43 nM 7.10
CHEMBL29950 Kd = 79.43 nM 7.10
CHEMBL440100 Kd = 169.82 nM 6.77
CHEMBL440101 Kd = 234.42 nM 6.63
CHEMBL280833 Kd = 239.88 nM 6.62
CHEMBL281488 Kd = 316.23 nM 6.50
CHEMBL31096 Kd = 354.81 nM 6.45
CHEMBL287409 Kd = 457.09 nM 6.34
CHEMBL284797 Kd = 537.03 nM 6.27
CHEMBL30905 Kd = 1000.0 nM 6.00
CHEMBL435357 Kd = 1659.59 nM 5.78
CHEMBL34577 Kd = 1995.26 nM 5.70
CHEMBL283236 Kd > 10000.0 nM -
CHEMBL30874 Kd > 10000.0 nM -