cariprazine [Ligand Id: 7671] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2028019 (Cariprazine, Fri-7000188, GED-129, MP-214, Reagila, RGH-188) |
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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 | Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 5.47 | pKi | 3414 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 5.47 | pKi | 3388.44 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay | B | 5.68 | pKi | 2100 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes | B | 5.68 | pKi | 2100 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO cell membranes after 3 hrs by liquid scintillation counting analysis | B | 7.75 | pKi | 17.78 | nM | Ki | J Med Chem (2013) 56: 9199-9221 [PMID:24138311] |
| GtoPdb | Binding affinity to human dopamine D2L receptor | - | 8.24 | pKi | 5.7 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3437-40 [PMID:22537450] |
| ChEMBL | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.84 | pKi | 1.45 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.84 | pKi | 1.45 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]spiperone from recombinant human D2L receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | B | 8.89 | pKi | 1.3 | nM | Ki | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| ChEMBL | Displacement of [3H]Spiperone from human D2S receptor expressed in CHO cells | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2017) 60: 6480-6515 [PMID:28421763] |
| ChEMBL | Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method | B | 9.31 | pKi | 0.49 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| ChEMBL | Displacement of [3H]-spiperone from recombinant human D2L receptor expressed in CHO cells | B | 9.31 | pKi | 0.49 | nM | Ki | Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D2L receptor expressed in CHO cells | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (2017) 60: 6480-6515 [PMID:28421763] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human D2-long receptor expressed in CHO cell membranes | B | 9.33 | pKi | 0.47 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human D2-short receptor expressed in CHO cell membranes | B | 9.39 | pKi | 0.41 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| ChEMBL | Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | B | 8.78 | pIC50 | 1.66 | nM | IC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay | F | 6.95 | pEC50 | 112.2 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | B | 8.46 | pEC50 | 3.47 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.63 | pEC50 | 2.37 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.63 | pEC50 | 2.34 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.99 | pEC50 | 1.02 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.99 | pEC50 | 1.02 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay | F | 9.35 | pEC50 | 0.45 | nM | EC50 | J Med Chem (2019) 62: 4755-4771 [PMID:30964661] |
| ChEMBL | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2019) 62: 4755-4771 [PMID:30964661] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes | B | 9.57 | pKi | 0.27 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assay | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | B | 10.02 | pKi | 0.1 | nM | Ki | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| GtoPdb | Binding affinity to human dopamine D3 receptor | - | 10.05 | pKi | 0.09 | nM | Ki | J Pharmacol Exp Ther (2010) 333: 328-40 [PMID:20093397] |
| ChEMBL | Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cells | B | 10.07 | pKi | 0.09 | nM | Ki | Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775] |
| ChEMBL | Displacement of [3H]Spiperone from dopamine D3 receptor (unknown origin) | B | 10.07 | pKi | 0.09 | nM | Ki | J Med Chem (2017) 60: 6480-6515 [PMID:28421763] |
| ChEMBL | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | F | 8.24 | pEC50 | 5.8 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | F | 8.24 | pEC50 | 5.75 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 6.29 | pKi | 507 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes | B | 6.96 | pKi | 110 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes | B | 5.1 | pKi | 7900 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential after 2 mins by patch clamp assay | B | 4.68 | pIC50 | 20720 | nM | IC50 | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells | B | 7.63 | pKi | 23.2 | nM | Ki | Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.4 | pKi | 4.01 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method | B | 8.51 | pKi | 3.1 | nM | Ki | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 8.59 | pKi | 2.6 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| ChEMBL | Displacement of [3H]OH-DPAT from recombinant human 5-HT1A receptor expressed in human HEK293 cells | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]-LSD from 5HT2A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 6.66 | pKi | 219.4 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-LSD from 5HT2A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 6.66 | pKi | 218.78 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method | B | 7.64 | pKi | 23 | nM | Ki | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293T cell membranes | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem (2017) 25: 3491-3499 [PMID:28495386] |
| ChEMBL | Displacement of [3H]-ketanserin from human 5HT2A receptor expressed in HEK293 cells by competitive binding assay | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in rat cortex tissue incubated for 30 mins by liquid scintillation counting method | B | 7.73 | pKi | 18.8 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| ChEMBL | Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in human HEK293 cells | B | 7.73 | pKi | 18.8 | nM | Ki | Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 6.7 | pKi | 198.2 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method | B | 6.95 | pKi | 111 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
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]
