(-)-N-porphynorapomorphine [Ligand Id: 969] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL225230 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells | B | 5.74 | pKd | 1816 | nM | Kd | J Med Chem (1996) 39: 850-859 [PMID:8632409] |
| ChEMBL | Affinity towards Dopamine receptor D1 | B | 5.82 | pKi | 1510 | nM | Ki | J Med Chem (1998) 41: 4385-4399 [PMID:9784114] |
| ChEMBL | Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assay | B | 6.31 | pKi | 490 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assay | B | 9 | pKi | 1 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 5.72 | pEC50 | 1884 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 5.73 | pEC50 | 1862.09 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 8.96 | pEC50 | 1.1 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 8.96 | pEC50 | 1.1 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum | B | 5.47 | pKi | 3410 | nM | Ki | J Med Chem (2008) 51: 983-987 [PMID:18251489] |
| ChEMBL | Displacement of [3H]SCH-23390 from rat dopamine D1 receptor | B | 6.14 | pKi | 730 | nM | Ki | J Med Chem (2007) 50: 171-181 [PMID:17228858] |
| ChEMBL | Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390 | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (1991) 34: 24-28 [PMID:1671415] |
| ChEMBL | Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (1990) 33: 1800-1805 [PMID:1971309] |
| ChEMBL | Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane | B | 6.19 | pIC50 | 640 | nM | IC50 | J Med Chem (1990) 33: 3122-3124 [PMID:2147956] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D2A expressed in COS7 cells | B | 7.7 | pKd | 20 | nM | Kd | J Med Chem (1996) 39: 850-859 [PMID:8632409] |
| ChEMBL | Affinity towards Dopamine receptor D2 | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1998) 41: 4385-4399 [PMID:9784114] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621] |
| ChEMBL | Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2004) 47: 6595-6602 [PMID:15588094] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8.93 | pEC50 | 1.18 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8.93 | pEC50 | 1.18 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 6.28 | pKd | 520 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 6.43 | pKd | 370 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. | B | 7.4 | pKd | 40 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. | B | 8.05 | pKd | 9 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D2 receptor low binding site in Sprague-Dawley rat striatum by scintillation counting | B | 7.27 | pKi | 54 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Displacement of [3H]raclopride from rat dopamine D2 receptor | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2007) 50: 171-181 [PMID:17228858] |
| ChEMBL | Displacement of [3H]neomonapride from dopamine D2 receptor in rat striatum | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2008) 51: 983-987 [PMID:18251489] |
| ChEMBL | Compound was evaluated for its ability to inhibit dopamine receptor D2 in rat striatum using [3H]-spiperone | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1991) 34: 24-28 [PMID:1671415] |
| ChEMBL | Binding affinity at rat striatal Dopamine receptor D2 using [3H]- piperone radioligand | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1990) 33: 1800-1805 [PMID:1971309] |
| ChEMBL | Displacement of [3H]domperidone from dopamine D2 receptor high binding site in Sprague-Dawley rat striatum by scintillation counting | B | 9.74 | pKi | 0.18 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Evaluated for the affinity against Dopamine receptor D2 in rat striatal membranes | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1988) 31: 1466-1471 [PMID:2968456] |
| ChEMBL | Binding affinity against Dopamine receptor D2 from rat brain corpus striatum membrane | B | 8.32 | pIC50 | 4.8 | nM | IC50 | J Med Chem (1990) 33: 3122-3124 [PMID:2147956] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621] |
| ChEMBL | Displacement of [3H]domperidone from human dopamine D3 receptor expressed in human HEK293 cells by scintillation counting | B | 9.36 | pKi | 0.44 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| L-Tyrosine hydroxylase /Tyrosine 3-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1969] [GtoPdb: 1243] [UniProtKB: P07101] | ||||||||
| ChEMBL | Inhibition of tyrosine hydroxylase | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2007) 50: 171-181 [PMID:17228858] |
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]
