tamsulosin [Ligand Id: 488] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL836 (HGP-0412, HIP-1402, HIP1402, Tamsulon, Tamsulosin) |
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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 | - | - | - |
FEBS Lett (1998) 422: 279-83 [PMID:9490024]; Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511]; Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]; J Pharmacol Exp Ther (2019) 371: 106-112 [PMID:31285236]; J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Br J Pharmacol (1999) 127: 252-8 [PMID:10369480] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
