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Assay Detail

CHEMBL663908

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

Functional
Effective concentration for the agonist in the isolated blood vessel using in vitro saphenous vein
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Tissue Saphenous vein
Confidence 1 — Organism
Curated By Expert

Target

Canis familiaris (CHEMBL373)
Type ORGANISM
Organism Canis lupus familiaris

Publication

Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)].
Cordi AA, Lacoste JM, Descombes JJ, Courchay C, Vanhoutte PM, Laubie M, Verbeuren TJ.
J Med Chem (1995) 38 : 4056 -4069
PubMed 7562941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 41 5.59 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133231 1 7.85
CHEMBL337879 1 7.64
CHEMBL340679 1 7.57
CHEMBL132119 1 7.16
CHEMBL130784 1 6.75
CHEMBL128582 1 6.62
CHEMBL98471 1 6.58
CHEMBL336331 1 6.52
CHEMBL131417 1 6.30
CHEMBL445329 1 6.10
CHEMBL336332 1 6.10
CHEMBL130853 1 5.89
CHEMBL338683 1 5.70
CHEMBL128574 1 5.68
CHEMBL131220 1 5.64
CHEMBL128593 1 5.64
CHEMBL336631 1 5.62
CHEMBL336521 1 5.57
CHEMBL130589 1 5.57
CHEMBL338616 1 5.54
CHEMBL335694 1 5.41
CHEMBL131539 1 5.41
CHEMBL130679 1 5.37
CHEMBL101340 1 5.29
CHEMBL128055 1 5.26
CHEMBL441833 1 5.22
CHEMBL131655 1 5.20
CHEMBL133579 1 5.15
CHEMBL131596 1 5.14
CHEMBL336970 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133231 EC50 = 14.0 nM 7.85
CHEMBL337879 EC50 = 23.0 nM 7.64
CHEMBL340679 EC50 = 27.0 nM 7.57
CHEMBL132119 EC50 = 70.0 nM 7.16
CHEMBL130784 EC50 = 180.0 nM 6.75
CHEMBL128582 EC50 = 240.0 nM 6.62
CHEMBL98471 EC50 = 260.0 nM 6.58
CHEMBL336331 EC50 = 300.0 nM 6.52
CHEMBL131417 EC50 = 500.0 nM 6.30
CHEMBL445329 EC50 = 800.0 nM 6.10
CHEMBL336332 EC50 = 800.0 nM 6.10
CHEMBL130853 EC50 = 1300.0 nM 5.89
CHEMBL338683 EC50 = 2000.0 nM 5.70
CHEMBL128574 EC50 = 2100.0 nM 5.68
CHEMBL128593 EC50 = 2300.0 nM 5.64
CHEMBL131220 EC50 = 2300.0 nM 5.64
CHEMBL336631 EC50 = 2400.0 nM 5.62
CHEMBL336521 EC50 = 2700.0 nM 5.57
CHEMBL130589 EC50 = 2700.0 nM 5.57
CHEMBL338616 EC50 = 2900.0 nM 5.54
CHEMBL335694 EC50 = 3900.0 nM 5.41
CHEMBL131539 EC50 = 3900.0 nM 5.41
CHEMBL130679 EC50 = 4300.0 nM 5.37
CHEMBL101340 EC50 = 5100.0 nM 5.29
CHEMBL128055 EC50 = 5500.0 nM 5.26
CHEMBL441833 EC50 = 6000.0 nM 5.22
CHEMBL131655 EC50 = 6300.0 nM 5.20
CHEMBL133579 EC50 = 7100.0 nM 5.15
CHEMBL131596 EC50 = 7300.0 nM 5.14
CHEMBL336970 EC50 = 8800.0 nM 5.06
CHEMBL131363 EC50 = 10000.0 nM 5.00
CHEMBL130044 EC50 = 11000.0 nM 4.96
CHEMBL414431 EC50 = 19000.0 nM 4.72
CHEMBL131553 EC50 = 25000.0 nM 4.60
CHEMBL130570 EC50 = 40000.0 nM 4.40
CHEMBL128420 EC50 = 44000.0 nM 4.36
CHEMBL129845 EC50 = 52000.0 nM 4.28
CHEMBL131240 EC50 = 52000.0 nM 4.28
CHEMBL130772 EC50 = 66000.0 nM 4.18
CHEMBL132951 EC50 = 75000.0 nM 4.12
CHEMBL334757 EC50 = 400000.0 nM -