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Assay Detail

CHEMBL648011

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

Binding
In vitro binding affinity towards alpha-1D adrenergic receptor of rat clone in radioligand binding assay
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1D adrenergic receptor (CHEMBL326)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.
J Med Chem (2004) 47 : 3220 -3235
PubMed 15163201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 5.95 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317912 1 7.51
CHEMBL112814 1 7.00
CHEMBL323402 1 6.72
CHEMBL326702 1 6.56
CHEMBL327116 1 6.47
CHEMBL110852 1 6.45
CHEMBL323004 1 6.44
CHEMBL111685 1 6.35
CHEMBL110976 1 6.32
CHEMBL432451 1 6.30
CHEMBL111682 1 6.16
CHEMBL111463 1 6.15
CHEMBL111771 1 6.01
CHEMBL110859 1 6.00
CHEMBL111734 1 6.00
CHEMBL111584 1 5.98
CHEMBL111496 1 5.97
CHEMBL111151 1 5.94
CHEMBL108804 1 5.90
CHEMBL109783 1 5.83
CHEMBL326862 1 5.80
CHEMBL111554 1 5.80
CHEMBL1076 DESGLYMIDODRINE -1.0 1 5.78
CHEMBL3350265 2 5.77
CHEMBL2111710 1 5.72
CHEMBL111537 1 5.69
CHEMBL322492 1 5.60
CHEMBL323440 1 5.57
CHEMBL325897 1 5.57
CHEMBL322082 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317912 Ki = 30.9 nM 7.51
CHEMBL112814 Ki = 100.0 nM 7.00
CHEMBL323402 Ki = 190.55 nM 6.72
CHEMBL326702 Ki = 275.42 nM 6.56
CHEMBL327116 Ki = 338.84 nM 6.47
CHEMBL110852 Ki = 354.81 nM 6.45
CHEMBL323004 Ki = 363.08 nM 6.44
CHEMBL111685 Ki = 446.68 nM 6.35
CHEMBL110976 Ki = 478.63 nM 6.32
CHEMBL432451 Ki = 501.19 nM 6.30
CHEMBL111682 Ki = 691.83 nM 6.16
CHEMBL111463 Ki = 707.95 nM 6.15
CHEMBL111771 Ki = 977.24 nM 6.01
CHEMBL110859 Ki = 1000.0 nM 6.00
CHEMBL111734 Ki = 1000.0 nM 6.00
CHEMBL111584 Ki = 1047.13 nM 5.98
CHEMBL111496 Ki = 1071.52 nM 5.97
CHEMBL111151 Ki = 1148.15 nM 5.94
CHEMBL108804 Ki = 1258.93 nM 5.90
CHEMBL109783 Ki = 1479.11 nM 5.83
CHEMBL111554 Ki = 1584.89 nM 5.80
CHEMBL326862 Ki = 1584.89 nM 5.80
CHEMBL1076 DESGLYMIDODRINE Ki = 1659.59 nM 5.78
CHEMBL3350265 Ki = 1698.24 nM 5.77
CHEMBL2111710 Ki = 1905.46 nM 5.72
CHEMBL111537 Ki = 2041.74 nM 5.69
CHEMBL3350265 Ki = 2137.96 nM 5.67
CHEMBL322492 Ki = 2511.89 nM 5.60
CHEMBL325897 Ki = 2691.53 nM 5.57
CHEMBL323440 Ki = 2691.53 nM 5.57
CHEMBL322082 Ki = 2884.03 nM 5.54
CHEMBL322042 Ki = 3019.95 nM 5.52
CHEMBL109827 Ki = 3019.95 nM 5.52
CHEMBL110751 Ki = 3311.31 nM 5.48
CHEMBL110975 Ki = 3630.78 nM 5.44
CHEMBL109755 Ki = 4265.8 nM 5.37
CHEMBL111412 Ki = 6456.54 nM 5.19
CHEMBL61006 PHENYLPROPANOLAMINE Ki = 8511.38 nM 5.07
CHEMBL324238 Ki < 10000.0 nM -
CHEMBL320353 Ki < 10000.0 nM -
CHEMBL442394 Ki < 10000.0 nM -
CHEMBL111536 Ki < 10000.0 nM -
CHEMBL109553 Ki < 10000.0 nM -
CHEMBL326437 Ki < 10000.0 nM -
CHEMBL111372 Ki < 10000.0 nM -
CHEMBL110860 Ki < 10000.0 nM -
CHEMBL109848 Ki < 10000.0 nM -
CHEMBL321644 Ki < 10000.0 nM -
CHEMBL111391 Ki < 10000.0 nM -
CHEMBL320765 Ki < 10000.0 nM -