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: 144-50 [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 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]
