tamsulosin [Ligand Id: 488] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL836 (HGP-0412, HIP1402, HIP-1402, Tamsulon, Tamsulosin)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • Alpha-1a adrenergic receptor in Rabbit [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • Alpha-1b adrenergic receptor in Hamster [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate F 9.54 pKd 0.29 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro antagonistic activity against alpha-1A receptor in dog prostate. F 9.54 pKd 0.29 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 8.4 pKi 3.98 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor B 9.72 pKi 0.19 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 640-644 [PMID:18055202]
ChEMBL Binding affinity to human cloned adrenergic alpha-1a receptor B 9.72 pKi 0.19 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3930-3934 [PMID:17517507]
ChEMBL Binding affinity to human cloned adrenergic alpha-1A receptor B 9.72 pKi 0.19 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3292-3297 [PMID:17452102]
ChEMBL Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand B 9.89 pKi 0.13 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand B 9.89 pKi 0.13 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells B 10.3 pKi 0.05 nM Ki Eur. J. Med. Chem. (2010) 45: 5800-5807 [PMID:20934789]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand B 10.54 pKi 0.03 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
GtoPdb - - 10.7 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
FEBS Lett (1998) 422: 279-83 [PMID:9490024];
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480];
Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511]
ChEMBL Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay F 8.66 pIC50 2.2 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
ChEMBL Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay F 9.49 pIC50 0.32 nM IC50 Eur J Med Chem (2020) 205: 112616-112616 [PMID:32949920]
ChEMBL Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay B 10.15 pEC50 0.07 nM EC50 Bioorg Med Chem (2016) 24: 5582-5591 [PMID:27658792]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor B 9.9 pKi 0.13 nM Ki J. Med. Chem. (1997) 40: 2674-2687 [PMID:9276013]
Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
ChEMBL Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay F 9.8 pKd 0.16 nM Kd J. Med. Chem. (1997) 40: 2674-2687 [PMID:9276013]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens F 9.47 pKd 0.34 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens F 9.47 pKd 0.34 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter B 9.89 pKi 0.13 nM Ki Eur. J. Med. Chem. (2011) 46: 3000-3012 [PMID:21549456]
ChEMBL In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A B 10.52 pKi 0.03 nM Ki J. Med. Chem. (2000) 43: 1586-1603 [PMID:10780916]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7 pKi 100 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity to human cloned adrenergic alpha-1b receptor B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3930-3934 [PMID:17517507]
ChEMBL Binding affinity to human cloned adrenergic alpha-1B receptor B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3292-3297 [PMID:17452102]
ChEMBL Displacement of [125I]HEAT from human recombinant adrenergic Alpha-1B receptor B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 640-644 [PMID:18055202]
ChEMBL Binding affinity towards cloned human alpha-1B adrenergic receptor was determined using [125]-HEAT as radioligand B 8.72 pKi 1.92 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 8.9 pKi 1.26 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 8.9 pKi 1.26 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells B 9.2 pKi 0.63 nM Ki Eur. J. Med. Chem. (2010) 45: 5800-5807 [PMID:20934789]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-1B adrenergic receptor using [3H]prazosin as radioligand B 9.21 pKi 0.61 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
GtoPdb - - 9.7 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]
ChEMBL Antagonist activity at human alpha1B receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay F 8.38 pIC50 4.2 nM IC50 Eur J Med Chem (2020) 205: 112616-112616 [PMID:32949920]
Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
ChEMBL In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1b expressed in LTK cell B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2000) 43: 1586-1603 [PMID:10780916]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL In vitro antagonism against Alpha-1B adrenergic receptor using phenylephrine (PE) challenge in rat spleen F 9.69 pKd 0.2 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro antagonistic activity against alpha-1B receptor in rat spleen. F 9.69 pKd 0.2 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 8.1 pKi 7.94 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [125I]HEAT from human recombinant adrenergic alpha1C receptor B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 640-644 [PMID:18055202]
ChEMBL Binding affinity to human cloned adrenergic alpha-1d receptor B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3930-3934 [PMID:17517507]
ChEMBL Binding affinity to human cloned adrenergic Alpha-1D receptor B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3292-3297 [PMID:17452102]
ChEMBL Displacement of [125I] HEAT from human alpha1D adrenergic receptor expressed in Chlorocebus aethiops COS1 cell membranes incubated for 60 mins by liquid scintillation counting analysis B 9.74 pKi 0.18 nM Ki J. Med. Chem. (2016) 59: 2989-3002 [PMID:26954848]
ChEMBL Binding affinity towards cloned human alpha-1D adrenergic receptor was determined using [125]-HEAT as radioligand B 9.74 pKi 0.18 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 9.8 pKi 0.16 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 9.8 pKi 0.16 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells B 10 pKi 0.1 nM Ki Eur. J. Med. Chem. (2010) 45: 5800-5807 [PMID:20934789]
GtoPdb - - 10.2 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-1D adrenergic receptor using [3H]prazosin as radioligand B 10.24 pKi 0.06 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL Antagonist activity at human full-length N-terminal SNAP-tagged alpha1D adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay F 8.85 pIC50 1.4 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
ChEMBL Antagonist activity at human alpha1D receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay F 9.82 pIC50 0.15 nM IC50 Eur J Med Chem (2020) 205: 112616-112616 [PMID:32949920]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL In vitro antagonism against Alpha-1D adrenergic receptor using phenylephrine (PE) challenge in rat aorta F 10.6 pKd 0.03 nM Kd J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
ChEMBL In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1d expressed in LTK cell B 10.15 pKi 0.07 nM Ki J. Med. Chem. (2000) 43: 1586-1603 [PMID:10780916]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand B 7.2 pKi 63 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand B 7.87 pKi 13.4 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Binding affinity towards rat alpha-2B adrenergic receptor was determined using [3H]yohimbine as radioligand B 7.1 pKi 80 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Binding affinity against rat Alpha-2B adrenergic receptor using [3H]rauwolscine as radioligand B 8.17 pKi 6.8 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand B 8.1 pKi 7.9 nM Ki J. Med. Chem. (1997) 40: 3141-3143 [PMID:9379432]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity towards recombinant human Dopamine receptor D2S was determined using [3H]spiperone as radioligand B 7.11 pKi 78 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
ChEMBL Binding affinity towards recombinant human Dopamine receptor D2L was determined using [3H]spiperone as radioligand B 7.89 pKi 13 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards recombinant human Dopamine receptor D3 was determined using [3H]spiperone as radioligand B 9.55 pKi 0.28 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards recombinant human Compound at 1 uM was tested for the inhibition of radioligand [3H]8-OH-DPAT binding to recombinant human 5-hydroxytryptamine 1A receptor was determined using [3H]8-OH-DPAT as radioligand B 9.1 pKi 0.79 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity towards recombinant human 5-hydroxytryptamine 7 receptor was determined using [3H]LSD as radioligand B 7.08 pKi 84 nM Ki J. Med. Chem. (2000) 43: 2183-2195 [PMID:10841797]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]