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Assay Detail

CHEMBL648102

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

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

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Alpha-1B adrenergic receptor (CHEMBL3122) ↗
Type SINGLE PROTEIN
Organism Mesocricetus auratus

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 5.61 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317912 — — 1 6.84
CHEMBL112814 — — 1 6.67
CHEMBL323402 — — 1 6.28
CHEMBL111685 — — 1 6.05
CHEMBL326702 — — 1 6.05
CHEMBL111496 — — 1 5.88
CHEMBL327116 — — 1 5.87
CHEMBL110976 — — 1 5.77
CHEMBL2111710 — — 1 5.70
CHEMBL111771 — — 1 5.70
CHEMBL111584 — — 1 5.69
CHEMBL108804 — — 1 5.60
CHEMBL109783 — — 1 5.53
CHEMBL111554 — — 1 5.33
CHEMBL1076 DESGLYMIDODRINE -1.0 1 5.16
CHEMBL109755 — — 1 5.13
CHEMBL111734 — — 1 5.09
CHEMBL61006 PHENYLPROPANOLAMINE 4.0 1 5.02
CHEMBL322492 — — 1 5.00
CHEMBL111412 — — 1 5.00
CHEMBL109827 — — 1 5.00
CHEMBL3350265 — — 2 4.98
CHEMBL110852 — — 1 -
CHEMBL111463 — — 1 -
CHEMBL323004 — — 1 -
CHEMBL442394 — — 1 -
CHEMBL320353 — — 1 -
CHEMBL110860 — — 1 -
CHEMBL321644 — — 1 -
CHEMBL324238 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317912 — Ki = 144.54 nM 6.84
CHEMBL112814 — Ki = 213.8 nM 6.67
CHEMBL323402 — Ki = 524.81 nM 6.28
CHEMBL326702 — Ki = 891.25 nM 6.05
CHEMBL111685 — Ki = 891.25 nM 6.05
CHEMBL111496 — Ki = 1318.26 nM 5.88
CHEMBL327116 — Ki = 1348.96 nM 5.87
CHEMBL110976 — Ki = 1698.24 nM 5.77
CHEMBL2111710 — Ki = 1995.26 nM 5.70
CHEMBL111771 — Ki = 1995.26 nM 5.70
CHEMBL111584 — Ki = 2041.74 nM 5.69
CHEMBL108804 — Ki = 2511.89 nM 5.60
CHEMBL109783 — Ki = 2951.21 nM 5.53
CHEMBL111554 — Ki = 4677.35 nM 5.33
CHEMBL1076 DESGLYMIDODRINE Ki = 6918.31 nM 5.16
CHEMBL109755 — Ki = 7413.1 nM 5.13
CHEMBL111734 — Ki = 8128.31 nM 5.09
CHEMBL61006 PHENYLPROPANOLAMINE Ki = 9549.93 nM 5.02
CHEMBL111412 — Ki = 10000.0 nM 5.00
CHEMBL109827 — Ki = 10000.0 nM 5.00
CHEMBL322492 — Ki = 10000.0 nM 5.00
CHEMBL3350265 — Ki = 10471.29 nM 4.98
CHEMBL322082 — Ki < 10000.0 nM -
CHEMBL3350265 — Ki < 10000.0 nM -
CHEMBL111682 — Ki < 10000.0 nM -
CHEMBL323440 — Ki < 10000.0 nM -
CHEMBL110859 — Ki < 10000.0 nM -
CHEMBL111537 — Ki < 10000.0 nM -
CHEMBL107726 — Ki < 10000.0 nM -
CHEMBL111391 — Ki < 10000.0 nM -
CHEMBL110751 — Ki < 10000.0 nM -
CHEMBL111151 — Ki < 10000.0 nM -
CHEMBL326862 — Ki < 10000.0 nM -
CHEMBL320589 — Ki < 10000.0 nM -
CHEMBL109848 — Ki < 10000.0 nM -
CHEMBL321644 — Ki < 10000.0 nM -
CHEMBL111372 — Ki < 10000.0 nM -
CHEMBL110860 — Ki < 10000.0 nM -
CHEMBL111463 — Ki < 10000.0 nM -
CHEMBL326437 — Ki < 10000.0 nM -
CHEMBL432451 — Ki < 10000.0 nM -
CHEMBL419369 — Ki < 10000.0 nM -
CHEMBL323004 — Ki < 10000.0 nM -
CHEMBL442394 — Ki < 10000.0 nM -
CHEMBL320353 — Ki < 10000.0 nM -
CHEMBL109553 — Ki < 10000.0 nM -
CHEMBL324238 — Ki < 10000.0 nM -
CHEMBL110975 — Ki < 10000.0 nM -
CHEMBL325897 — Ki < 10000.0 nM -
CHEMBL110852 — Ki < 10000.0 nM -