MK-212 [Ligand Id: 165] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL269521 (MK-212) |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Binding affinity at rat Dopamine receptor D1 by [3H]SCH-23390 displacement. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity against rat Dopamine receptor D2. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 6.1 | pKd | 794.33 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 1A receptor by [3H]WB-4101 displacement. | B | 6.69 | pKi | 202 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone. | B | 5.22 | pKi | 6000 | nM | Ki | J Med Chem (1985) 28: 945-948 [PMID:4009617] |
| ChEMBL | Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT | B | 5.44 | pKi | 3630 | nM | Ki | J Med Chem (1985) 28: 945-948 [PMID:4009617] |
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement. | B | 6.75 | pKi | 178 | nM | Ki | J Med Chem (1989) 32: 1052-1056 [PMID:2565400] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 4.68 | pKi | 21000 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 4.68 | pKi | 20892.96 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| GtoPdb | - | - | 6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay | F | 5.92 | pEC50 | 1202.26 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay | F | 5.92 | pEC50 | 1200 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay | F | 6.37 | pEC50 | 426.58 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay | F | 6.38 | pEC50 | 420 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 5.47 | pKi | 3388.44 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| GtoPdb | - | - | 7 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Br J Pharmacol (2003) 140: 277-84 [PMID:12970106]; Synapse (2000) 35: 144-150 [PMID:10611640] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay | F | 6.79 | pEC50 | 162.18 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay | F | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay | F | 7.55 | pEC50 | 28.18 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay | F | 7.55 | pEC50 | 28 | nM | EC50 | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Br J Pharmacol (2003) 140: 277-84 [PMID:12970106] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
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]
