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ChEMBL ligand: CHEMBL629 (Amitid, Amitril, Amitriptyline, Damitriptyline, Elavil, Endep, Etrafon-A, Etrafon-Forte, Flavyl, Laroxyl, Limbitrol, Proheptadiene, Seroten, Triptanol) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
GtoPdb | - | - | 8.2 | pKi | - | - | - | Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
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 | 8.25 | pKi | 5.6 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.85 | pIC50 | 14 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor | B | 10.7 | pIC50 | 0.02 | nM | IC50 | J Med Chem (1999) 42: 3154-3162 [PMID:10447960] |
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 | 7.38 | pKi | 42 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.12 | pIC50 | 76 | 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 | 7.28 | pKi | 52 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.98 | pIC50 | 105 | 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 | 6.88 | pKi | 132 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.45 | pIC50 | 351 | 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 | 8.43 | pKi | 3.69 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 8.09 | pIC50 | 8.08 | 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 | 8.07 | pKi | 8.6 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 7.23 | pIC50 | 59 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.75 | pKi | 178 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells | B | 7.05 | pKi | 89 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.45 | pIC50 | 355 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.47 | pKi | 336 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells | B | 6.71 | pKi | 196 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6 | pIC50 | 1009 | 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 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 6.69 | pKi | 206 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.21 | pKi | 62 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 6.74 | pIC50 | 182 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells | B | 6.77 | pKi | 170 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | B | 5.21 |