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Assay Detail

CHEMBL648415

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Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL ↗
47
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL319) ↗
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 47 6.41 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109783 — — 1 7.92
CHEMBL111771 — — 1 7.65
CHEMBL108804 — — 1 7.44
CHEMBL323004 — — 1 7.34
CHEMBL111496 — — 1 7.33
CHEMBL110975 — — 1 7.08
CHEMBL2111710 — — 1 7.04
CHEMBL321644 — — 1 6.91
CHEMBL111734 — — 1 6.89
CHEMBL326702 — — 1 6.87
CHEMBL110751 — — 1 6.78
CHEMBL111554 — — 1 6.71
CHEMBL111463 — — 1 6.69
CHEMBL111685 — — 1 6.57
CHEMBL111584 — — 1 6.56
CHEMBL322042 — — 1 6.51
CHEMBL323440 — — 1 6.41
CHEMBL322082 — — 1 6.35
CHEMBL109755 — — 1 6.34
CHEMBL111151 — — 1 6.32
CHEMBL110859 — — 1 6.30
CHEMBL110976 — — 1 6.30
CHEMBL109848 — — 1 6.28
CHEMBL325897 — — 1 6.27
CHEMBL111372 — — 1 6.15
CHEMBL432451 — — 1 6.15
CHEMBL109553 — — 1 6.10
CHEMBL320765 — — 1 6.10
CHEMBL3350265 — — 2 6.08
CHEMBL111682 — — 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109783 — Ki = 12.02 nM 7.92
CHEMBL111771 — Ki = 22.39 nM 7.65
CHEMBL108804 — Ki = 36.31 nM 7.44
CHEMBL323004 — Ki = 45.71 nM 7.34
CHEMBL111496 — Ki = 46.77 nM 7.33
CHEMBL110975 — Ki = 83.18 nM 7.08
CHEMBL2111710 — Ki = 91.2 nM 7.04
CHEMBL321644 — Ki = 123.03 nM 6.91
CHEMBL111734 — Ki = 128.82 nM 6.89
CHEMBL326702 — Ki = 134.9 nM 6.87
CHEMBL110751 — Ki = 165.96 nM 6.78
CHEMBL111554 — Ki = 194.98 nM 6.71
CHEMBL111463 — Ki = 204.17 nM 6.69
CHEMBL111685 — Ki = 269.15 nM 6.57
CHEMBL111584 — Ki = 275.42 nM 6.56
CHEMBL322042 — Ki = 309.03 nM 6.51
CHEMBL323440 — Ki = 389.05 nM 6.41
CHEMBL322082 — Ki = 446.68 nM 6.35
CHEMBL109755 — Ki = 457.09 nM 6.34
CHEMBL111151 — Ki = 478.63 nM 6.32
CHEMBL110859 — Ki = 501.19 nM 6.30
CHEMBL110976 — Ki = 501.19 nM 6.30
CHEMBL109848 — Ki = 524.81 nM 6.28
CHEMBL325897 — Ki = 537.03 nM 6.27
CHEMBL432451 — Ki = 707.95 nM 6.15
CHEMBL111372 — Ki = 707.95 nM 6.15
CHEMBL320765 — Ki = 794.33 nM 6.10
CHEMBL109553 — Ki = 794.33 nM 6.10
CHEMBL3350265 — Ki = 831.76 nM 6.08
CHEMBL111682 — Ki = 831.76 nM 6.08
CHEMBL324238 — Ki = 933.25 nM 6.03
CHEMBL107726 — Ki = 1000.0 nM 6.00
CHEMBL3350265 — Ki = 1148.15 nM 5.94
CHEMBL111537 — Ki = 1148.15 nM 5.94
CHEMBL322492 — Ki = 1348.96 nM 5.87
CHEMBL419369 — Ki = 1380.38 nM 5.86
CHEMBL442394 — Ki = 1698.24 nM 5.77
CHEMBL111391 — Ki = 1698.24 nM 5.77
CHEMBL1076 DESGLYMIDODRINE Ki = 1995.26 nM 5.70
CHEMBL110852 — Ki = 2951.21 nM 5.53
CHEMBL61006 PHENYLPROPANOLAMINE Ki = 9772.37 nM 5.01
CHEMBL111412 — Ki < 10000.0 nM -
CHEMBL320589 — Ki < 10000.0 nM -
CHEMBL320353 — Ki < 10000.0 nM -
CHEMBL111536 — Ki < 10000.0 nM -
CHEMBL326437 — Ki < 10000.0 nM -
CHEMBL110860 — Ki < 10000.0 nM -