cariprazine [Ligand Id: 7671] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2028019 (Cariprazina, 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 D1 receptor in HEK293 cell membranes by scintillation counting method | B | 5.53 | pKi | 2920 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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]N-methylspiperone from human D2 receptor in HEK293 cell membranes measured after 60 mins by scintillation counting method | B | 9.11 | pKi | 0.78 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 | Modulation of human D2L receptor | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563] |
| 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]-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 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 in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.87 | pEC50 | 1.35 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.87 | pEC50 | 1.35 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.87 | pEC50 | 1.35 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.87 | pEC50 | 1.34 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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] |
| ChEMBL | Partial agonist activity at human D2 receptor assessed as increase in cAMP accumulation | B | 9.74 | pEC50 | 0.18 | nM | EC50 | J Med Chem (2021) 64: 8710-8726 [PMID:34110150] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| 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]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]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]-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]N-methylspiperone from human D3 receptor in HEK293 cell membranes measured after 60 mins by scintillation counting method | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 | Partial agonist activity at human D3 receptor assessed as inhibition constant | B | 10.07 | pKi | 0.09 | nM | Ki | J Med Chem (2021) 64: 8710-8726 [PMID:34110150] |
| ChEMBL | Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis | F | 8.69 | pIC50 | 2.02 | nM | IC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis | F | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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] |
| ChEMBL | Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.72 | pEC50 | 1.91 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.72 | pEC50 | 1.89 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 D4 receptor in HEK293 cell membranes by scintillation counting method | B | 6.63 | pKi | 233 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 | Binding affinity to 5-HT1AR (unknown origin) assessed as inhibition constant | B | 8.51 | pKi | 3.1 | nM | Ki | Eur J Med Chem (2022) 235: 114319-114319 [PMID:35367707] |
| 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] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in HEK293 cell membranes by scintillation counting method | B | 8.74 | pKi | 1.81 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]-5-HT from 5HT2A receptor in HEK293 cell membranes by scintillation counting method | B | 6.25 | pKi | 568 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 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 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 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] |
| 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] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]-5-HT from 5HT2B receptor in HEK293 cell membranes by scintillation counting method | B | 9.82 | pKi | 0.15 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]-5-HT from 5HT2C receptor in HEK293 cell membranes by scintillation counting method | B | 6.66 | pKi | 221.1 | nM | Ki | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 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]
