ergotamine [Ligand Id: 149] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL442 (Ergotamina, Ergotamine, NSC-95090)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-hydroxytryptamine receptor 4 in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
  • 5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • Adenylate cyclase in Arthrospira platensis [ChEMBL: CHEMBL5755] [UniProtKB: O32393]
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  • 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 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]
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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 Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • ABCB1/ATP-dependent translocase ABCB1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • ATP-dependent translocase ABCB1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • CCK1 receptor/Cholecystokinin receptor type A in Mouse [ChEMBL: CHEMBL2798] [GtoPdb: 76] [UniProtKB: O08786]
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  • D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • CCK2 receptor/Gastrin/cholecystokinin type B receptor in Mouse [ChEMBL: CHEMBL2854] [GtoPdb: 77] [UniProtKB: P56481]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
  • 5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
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  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 9.35 pKi 0.44 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 9.11 pIC50 0.77 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin) B 8.51 pKi 3.1 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin) B 8.52 pKi 3.02 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting B 8.68 pKi 2.1 nM Ki Bioorg Med Chem Lett (2011) 21: 6714-6723 [PMID:21982496]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 10.04 pKi 0.09 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 9.7 pIC50 0.2 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Displacement of [3H]5-carboximidotryptamine from 5-HT1D receptor after 1.5 hrs by scintillation counting B 8.22 pKi 6 nM Ki Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583]
ChEMBL Displacement of [3H]GR125743 from recombinant human 5-HT1D receptor expressed in HEK cells by scintillation counting B 8.37 pKi 4.3 nM Ki Bioorg Med Chem Lett (2011) 21: 6714-6723 [PMID:21982496]
ChEMBL Displacement of [3H]5-CT from 5-HT1D receptor (unknown origin) B 8.58 pKi 2.63 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]5-CT from 5-HT1D receptor (unknown origin) B 8.66 pKi 2.2 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1D receptor B 9.1 pKi 0.8 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
GtoPdb - - 9.1 pKi 0.8 nM Ki J Med Chem (2000) 43: 1011-8 [PMID:10715164]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.73 pKi 1.85 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.19 pIC50 6.49 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay F 8.1 pEC50 7.94 nM EC50 ACS Med Chem Lett (2024) 15: 337-339 [PMID:38505858]
ChEMBL Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay F 8.14 pEC50 7.3 nM EC50 ACS Med Chem Lett (2024) 15: 337-339 [PMID:38505858]
5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 8 pKi - - - Circulation (2000) 102: 2836-41 [PMID:11104741]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.66 pKi 2.2 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Circulation (2000) 102: 2836-41 [PMID:11104741]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.46 pIC50 3.46 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.54 pKi 29 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.25 pIC50 56 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909]
GtoPdb - - 7.9 pKi - - - Circulation (2000) 102: 2836-41 [PMID:11104741]
5-hydroxytryptamine receptor 4 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 6.58 pKi 264 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 5.8 pIC50 1584 nM IC50 DrugMatrix in vitro pharmacology data
5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity for rodent 5-hydroxytryptamine 5A receptor B 7.4 pKi 40 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor B 7.66 pKi 22 nM Ki J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) B 7.81 pKi 15.49 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting B 7.85 pKi 14 nM Ki Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583]
GtoPdb - - 8.7 pKi - - - FEBS Lett (1994) 355: 242-6 [PMID:7988681];
Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb - - 8.4 pKi - - - Mol Pharmacol (1993) 43: 313-9 [PMID:8450829];
Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685];
FEBS Lett (1995) 377: 451-6 [PMID:8549774]
5-HT5A receptor in Rat [GtoPdb: 10] [UniProtKB: P35364]
GtoPdb - - 8.2 pKi - - - Proc Natl Acad Sci USA (1993) 90: 3452-6 [PMID:7682702]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 8.6 pKi - - - Mol Pharmacol (1998) 54: 577-83 [PMID:9730917];
Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 9.02 pKi 0.95 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.69 pIC50 2.04 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8.6 pKi - - - Neuropharmacology (1997) 36: 713-20 [PMID:9225298];
J Neurochem (1998) 71: 2169-77 [PMID:9798944];
Mol Pharmacol (1998) 54: 577-83 [PMID:9730917]
Adenylate cyclase in Arthrospira platensis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5755] [UniProtKB: O32393]
ChEMBL Inhibition of Spirulina platensis adenylyl cyclase assessed as cAMP level by cAMP immunogenic assay B 4.15 pIC50 70000 nM IC50 J Med Chem (2008) 51: 4456-4464 [PMID:18630896]
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.49 pKi 3.26 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.09 pIC50 8.06 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.34 pKi 4.55 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.09 pIC50 8.21 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.62 pKi 24 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.31 pIC50 49 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 9.1 pKi 0.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.67 pIC50 2.12 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 8.76 pKi 1.75 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 8.42 pIC50 3.84 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 8.74 pKi 1.81 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 7.92 pIC50 12 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells F 4 pKi 98900 nM Ki Mol Pharmacol (2002) 61: 964-973 [PMID:11961113]
ChEMBL TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells F 4.85 pKi 14250 nM Ki Mol Pharmacol (2002) 61: 964-973 [PMID:11961113]
ATP-dependent translocase ABCB1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells F 4.74 pKi 18000 nM Ki J Pharmacol Exp Ther (2002) 303: 323-332 [PMID:12235267]
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 5.62 pKi 2392 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 5.38 pIC50 4142 nM IC50 DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 5.72 pKi 1898 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 5.56 pIC50 2761 nM IC50 DrugMatrix in vitro pharmacology data
CCK1 receptor/Cholecystokinin receptor type A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2798] [GtoPdb: 76] [UniProtKB: O08786]
ChEMBL Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes B 4.47 pIC50 34000 nM IC50 Bioorg Med Chem Lett (1992) 2: 9-12
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) B 6 pIC50 1000 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.06 pKi 864 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.76 pIC50 1728 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.84 pKi 1.43 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.37 pIC50 4.3 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8.83 pKi 1.46 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8.37 pIC50 4.31 nM IC50 DrugMatrix in vitro pharmacology data
CCK2 receptor/Gastrin/cholecystokinin type B receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2854] [GtoPdb: 77] [UniProtKB: P56481]
ChEMBL Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKB in mouse fore brain membranes B 4.77 pIC50 17000 nM IC50 Bioorg Med Chem Lett (1992) 2: 9-12
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 5.51 pIC50 3064 nM IC50 DrugMatrix in vitro pharmacology data
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.5 pIC50 3160 nM IC50 DrugMatrix in vitro pharmacology data
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.19 pIC50 6499 nM IC50 DrugMatrix in vitro pharmacology data
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 6.3 pKi - - - Proc Natl Acad Sci USA (1992) 89: 5517-21 [PMID:1608964];
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 6.8 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT1F receptor in Rat [GtoPdb: 5] [UniProtKB: P30940]
GtoPdb - - 7.3 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 2184-8 [PMID:8384716]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 7.3 pKi - - - Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]