MK-212 [Ligand Id: 165] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL269521 (MK-212)
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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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 B 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 B 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 B 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]