benzatropine [Ligand Id: 7601] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1201203 (Benzatropina, Benzatropine, Benztropine, Cobrentin, NK-02) |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.24 | pKi | 57 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.85 | pIC50 | 142 | 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 | 7.39 | pKi | 41 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.13 | pIC50 | 74 | 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 | 7.59 | pKi | 26 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.28 | pIC50 | 52 | 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 | 6.69 | pKi | 204 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.26 | pIC50 | 544 | 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 | 7.52 | pKi | 30 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.19 | pIC50 | 65 | 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 | 7.24 | pKi | 57 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.4 | pIC50 | 395 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 6.65 | pKi | 222 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 6.18 | pIC50 | 654 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.71 | pKi | 193 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]WIN-35428 from monkey dopamine transporter | B | 6.51 | pIC50 | 312 | nM | IC50 | J Med Chem (1994) 37: 2001-2010 [PMID:8027983] |
| ChEMBL | Inhibition of [3H]WIN-35428 binding to the dopamine transporter in the cynomolgus (macaca fascicularis) monkey caudate-putamen. | B | 6.51 | pIC50 | 312 | nM | IC50 | J Med Chem (1996) 39: 371-379 [PMID:8558504] |
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.61 | pIC50 | 243 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Binding affinity against Dopamine transporter using [125]RTI-55 | B | 6.63 | pKi | 237 | nM | Ki | J Med Chem (2001) 44: 3937-3945 [PMID:11689080] |
| ChEMBL | Displacement of [3H]WIN-35428 binding to the dopamine transporter (DAT) in Rat Caudate Putamen | B | 6.93 | pKi | 118 | nM | Ki | J Med Chem (1997) 40: 851-857 [PMID:9083473] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen | B | 6.93 | pKi | 118 | nM | Ki | J Med Chem (1994) 37: 2258-2261 [PMID:8057273] |
| ChEMBL | Displacement of [3H]WIN-35428 binding to the dopamine transporter in rat caudate putamen tissue. | B | 6.93 | pKi | 118 | nM | Ki | J Med Chem (1999) 42: 3502-3509 [PMID:10479283] |
| ChEMBL | Inhibition of [3H]WIN-35428 binding to the cocaine binding site on the dopamine transporter (DAT) in synaptosomal membrane preparations from rat striatal tissue | B | 6.93 | pKi | 118 | nM | Ki | J Med Chem (2003) 46: 1456-1464 [PMID:12672245] |
| ChEMBL | Affinity for rat dopamine transporter using [3H]WIN-35428 displacement. | B | 6.93 | pKi | 118 | nM | Ki | J Med Chem (1995) 38: 3933-3940 [PMID:7562926] |
| GtoPdb | Displacement of [3H]WIN35,428 binding to homogenised rat caudate putamen. | - | 6.93 | pKi | 118 | nM | Ki | J Med Chem (1995) 38: 3933-40 [PMID:7562926] |
| ChEMBL | Binding affinity to dopamine transporter (DAT) using [3H]WIN-35428 as a radioligand | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2000) 43: 4151-4159 [PMID:11063611] |
| ChEMBL | Inhibition of [3H]dopamine uptake in rat caudate putamen tissue. | F | 6.39 | pIC50 | 403 | nM | IC50 | J Med Chem (1999) 42: 3502-3509 [PMID:10479283] |
| ChEMBL | [3H]-Dopamine uptake inhibition in rat caudate putamen | F | 6.39 | pIC50 | 403 | nM | IC50 | J Med Chem (1997) 40: 851-857 [PMID:9083473] |
| ChEMBL | Inhibition of [3H]dopamine uptake in rat caudate putamen. | F | 6.39 | pIC50 | 403 | nM | IC50 | J Med Chem (1995) 38: 3933-3940 [PMID:7562926] |
| ChEMBL | Inhibition of [3H]dopamine uptake into rat striatal synaptosomes | F | 6.39 | pIC50 | 403 | nM | IC50 | J Med Chem (2005) 48: 3337-3343 [PMID:15857139] |
| ChEMBL | Ability to inhibit binding of [3H]WIN-35428 to dopamine transporter in rat caudate putamen | B | 6.93 | pIC50 | 118 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 823-827 [PMID:11277529] |
| ChEMBL | Displacement of [3H]WIN-35428 from Dopamine transporter of rat caudate putamen | B | 6.93 | pIC50 | 118 | nM | IC50 | J Med Chem (2005) 48: 3337-3343 [PMID:15857139] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 9.43 | pKi | 0.37 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 8.5 | pIC50 | 3.18 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.93 | pKi | 1185 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.92 | pIC50 | 1206 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.88 | pKi | 0.13 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.26 | pIC50 | 0.54 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| GtoPdb | Displacement binding experiment using homogenised rat caudate putamen. | - | 9.02 | pKi | 0.95 | nM | Ki | J Med Chem (1995) 38: 3933-40 [PMID:7562926] |
| ChEMBL | Affinity for rat M1 acetylcholine receptor using [3H]pirenzepine displacement. | B | 9.02 | pKi | 0.95 | nM | Ki | J Med Chem (1995) 38: 3933-3940 [PMID:7562926] |
| ChEMBL | Displacement of [3H]pirenzepine binding at Muscarinic acetylcholine receptor M1 in rat brain P2 membranes. | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1997) 40: 851-857 [PMID:9083473] |
| ChEMBL | Binding affinity against Muscarinic receptor from rat brain membranes using [3H]pirenzepine | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (2001) 44: 3937-3945 [PMID:11689080] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.44 | pKi | 3.67 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at human recombinant muscarinic receptor M2 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins | F | 7.2 | pIC50 | 63.1 | nM | IC50 | ACS Med Chem Lett (2021) 12: 155-161 [PMID:33488977] |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8 | pIC50 | 10 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Affinity for rat M1 acetylcholine receptor using [3H]-AF DX 384 displacement. | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (1995) 38: 3933-3940 [PMID:7562926] |
| GtoPdb | Displacement binding assay using homogenised rat caudate putamen. | - | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (1995) 38: 3933-40 [PMID:7562926] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.57 | pKi | 0.27 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins | F | 7.7 | pIC50 | 19.95 | nM | IC50 | ACS Med Chem Lett (2021) 12: 155-161 [PMID:33488977] |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.89 | pIC50 | 1.28 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.48 | pKi | 0.33 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins | F | 8.3 | pIC50 | 5.01 | nM | IC50 | ACS Med Chem Lett (2021) 12: 155-161 [PMID:33488977] |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.62 | pIC50 | 2.38 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.84 | pKi | 1.45 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.69 | pIC50 | 2.02 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.86 | pKi | 1379 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.86 | pIC50 | 1391 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor 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 | 8.16 | pKi | 6.97 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 7.62 | pIC50 | 24 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor 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 | 6.9 | pKi | 127 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.7 | pIC50 | 200 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor 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 | 7.49 | pKi | 32 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 7.21 | pIC50 | 61 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.89 | pKi | 1294 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.55 | pIC50 | 2788 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Binding affinity of [3H]citalopram for serotonin transporter in monkey | B | 4.62 | pIC50 | 24100 | nM | IC50 | J Med Chem (1994) 37: 2001-2010 [PMID:8027983] |
| ChEMBL | Inhibition of [3H]citalopram binding to the serotonin transporter in the cynomolgus (macaca fascicularis) monkey caudate-putamen. | B | 4.62 | pIC50 | 24100 | nM | IC50 | J Med Chem (1996) 39: 371-379 [PMID:8558504] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Binding affinity against serotonin transporter using [125]RTI-55 | B | 5.29 | pKi | 5150 | nM | Ki | J Med Chem (2001) 44: 3937-3945 [PMID:11689080] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 7.23 | pKi | 59 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 6.86 | pIC50 | 139 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| B0AT1 in Human [GtoPdb: 939] [UniProtKB: Q695T7] | ||||||||
| GtoPdb | - | - | 4.36 | pIC50 | 44000 | nM | IC50 | Br J Pharmacol (2017) 174: 468-482 [PMID:28176326] |
ChEMBL data shown on this page come from version 34:
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]
