bromocriptine [Ligand Id: 35] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL493 (2-bromo-.alpha.-ergocryptine, Bromergocryptine, Bromocriptina, Bromocriptine, CB-154, Ergocryptine, 2-bromo-, Parlodel, SANDOZ 15-754)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
There should be some charts here, you may need to enable JavaScript!
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
There should be some charts here, you may need to enable JavaScript!
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
There should be some charts here, you may need to enable JavaScript!
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
There should be some charts here, you may need to enable JavaScript!
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.55 pKi 2.82 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.16 pIC50 6.96 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.71 pKi 1.96 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.45 pIC50 3.55 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.82 pKi 15 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.52 pIC50 30 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 8.26 pKi 5.53 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 7.82 pIC50 15 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 7.5 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.8 pKi 16 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.46 pIC50 35 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 7.12 pKi 76 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.6 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.28 pIC50 520 nM IC50 DrugMatrix in vitro pharmacology data
synuclein alpha/Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840]
ChEMBL Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 6 days by thioflavin S based fluorescence assay B 4.61 pIC50 24700 nM IC50 Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 5.82 pKi 1521 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 5.64 pIC50 2281 nM IC50 DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 5.86 pKi 1386 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 5.62 pIC50 2400 nM IC50 DrugMatrix in vitro pharmacology data
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) B 5.7 pIC50 2000 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.84 pKi 1444 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.54 pIC50 2889 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [125]iodosulpride from human recombinant dopamine D2L receptor expressed in CHO cells after 30 mins B 7.82 pKi 15 nM Ki J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL Displacement of [125]iodosulpride from human recombinant dopamine D2L receptor expressed in CHO cells after 30 mins B 7.83 pKi 14.79 nM Ki J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170. B 8 pKi 10 nM Ki J Med Chem (1997) 40: 639-646 [PMID:9057850]
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Neuroreport (1995) 6: 329-332 [PMID:7756621]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) assessed as inhibition constant B 9.21 pKi 0.62 nM Ki RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 9.28 pKi 0.53 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.8 pIC50 1.58 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 9.3 pEC50 0.5 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. B 7.77 pKd 17 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. B 8.1 pKd 8 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. B 8.1 pKd 8 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. B 8.4 pKd 4 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
GtoPdb - - 7.3 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT. B 7.06 pKi 87 nM Ki J Med Chem (1997) 40: 639-646 [PMID:9057850]
GtoPdb - - 8.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Neuroreport (1995) 6: 329-332 [PMID:7756621]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 9.69 pKi 0.2 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 9.22 pIC50 0.6 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb - - 7.1 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
Genome polyprotein in Zika virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523954] [UniProtKB: A0A024AXB9]
ChEMBL Inhibition of Zika virus NS2B-NS3 protease B 4.67 pIC50 21600 nM IC50 Bioorg Med Chem Lett (2020) 30: 126965-126965 [PMID:31980339]
ChEMBL Inhibition of N-terminal His6-tagged Zika virus NS2B (49 to 95 residues) - NS3 (1 to 170 residues) protease domain expressed in Escherichia coli Bl21(DE3) using Bz-Nle-Lys-Lys-Arg-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by fluorescence based assay B 4.88 pIC50 13040 nM IC50 Eur J Med Chem (2019) 180: 536-545 [PMID:31344613]
ChEMBL Inhibition of NS2B-NS3 protease in Zika virus Puerto Rico/PRVABC5 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-induced cytopathic effect preincubated with cells for 2 hrs followed by compound wash out and subsequent virus addition along with compound and measured after 6 days by inverted light microscopy B 4.88 pEC50 13040 nM EC50 J Med Chem (2020) 63: 470-489 [PMID:31549836]
ChEMBL Inhibition of Zika virus NS2B-NS3 protease by cell based assay B 4.89 pEC50 13000 nM EC50 Bioorg Med Chem Lett (2020) 30: 126965-126965 [PMID:31980339]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells F 5.4 pKi 3960 nM Ki Mol Pharmacol (2002) 61: 964-973 [PMID:11961113]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells F 5.55 pKi 2810 nM Ki Mol Pharmacol (2002) 61: 964-973 [PMID:11961113]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells F 5.19 pKi 6390 nM Ki J Pharmacol Exp Ther (2002) 303: 323-332 [PMID:12235267]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells F 5.13 pKi 7480 nM Ki J Pharmacol Exp Ther (2002) 303: 323-332 [PMID:12235267]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT. B 7.62 pKi 24 nM Ki J Med Chem (1997) 40: 639-646 [PMID:9057850]
GtoPdb - - 7.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 8.49 pKi 3.22 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 8.25 pIC50 5.63 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.5 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 7.33 pKi 47 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 6.99 pIC50 103 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8 pKi 10 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 7.44 pIC50 36 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 8.75 pEC50 1.78 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 7.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.28 pKi 5.29 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.08 pIC50 8.32 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 6.1 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.56 pKi 278 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.27 pIC50 532 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at 5HT2C receptor VGV isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 5.8 pEC50 1584.89 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor B 7.3 pKi <50 nM Ki J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
GtoPdb - - 7.5 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8 pKi 10 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.66 pIC50 22 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.5 pKi - - - J Neurochem (1998) 71: 2169-77 [PMID:9798944]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 8 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 8 pKi - - - J Biol Chem (1993) 268: 18200-4 [PMID:8394362]
D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 6.4 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 6.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Nature (1991) 350: 614-9 [PMID:1826762]

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]