metoclopramide [Ligand Id: 241] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL86 (Clopra-"Yellow", Maxolon, Metoclopramide, Clopra, Reglan)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor in Mouse [GtoPdb: 215] [UniProtKB: P61168]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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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-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of guinea pig acetylcholinesterase B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (1993) 36: 572-579 [PMID:8496937]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity was evaluated by Alpha-1 adrenergic receptor in calf cortex by displacing prazosin B 5 pKd <5 - pKD J. Med. Chem. (1995) 38: 2326-2330 [PMID:7608898]
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 5.99 pKi 1020 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.57 pIC50 2721 nM IC50 DrugMatrix in vitro pharmacology data
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.1 pIC50 800 nM IC50 DrugMatrix in vitro pharmacology data
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Binding affinity was evaluated by Dopamine receptor D1 agonism in the calf striatum by displacing SCH 23390 B 5 pKd <5 - pKD J. Med. Chem. (1995) 38: 2326-2330 [PMID:7608898]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting. B 7.19 pKi 64 nM Ki US-9132134-B2. Methods for treating GI tract disorders (2015)
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.38 pKi 42 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.9 pIC50 127 nM IC50 DrugMatrix in vitro pharmacology data
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity was evaluated by Dopamine receptor D2 agonism in the calf striatum by displacing spiperone B 7.1 pKd 7.1 - pKD J. Med. Chem. (1995) 38: 2326-2330 [PMID:7608898]
ChEMBL Compound was evaluated for the binding affinity at Dopamine receptor D2 B 7.1 pKi 80 nM Ki J. Med. Chem. (1995) 38: 2326-2330 [PMID:7608898]
D2 receptor in Mouse [GtoPdb: 215] [UniProtKB: P61168]
GtoPdb - - 7.54 pKi 28.8 nM Ki J. Pharmacol. Exp. Ther. (1998) 287: 725-32 [PMID:9808703]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand B 6.52 pKi 303 nM Ki J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
ChEMBL Binding affinity against Dopamine receptor D2 using [3H]spiperone as radioligand in rat striatum B 6.55 pKi 285 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 795-798
ChEMBL Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI B 6.63 pKi 235 nM Ki J. Med. Chem. (1992) 35: 2355-2363 [PMID:1535660]
ChEMBL Binding affinity to dopamine receptor D2 B 6.95 pKi 113 nM Ki J. Med. Chem. (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI B 6.98 pKi 104 nM Ki J. Med. Chem. (1992) 35: 2355-2363 [PMID:1535660]
ChEMBL Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor B 6.09 pIC50 820 nM IC50 J. Med. Chem. (1992) 35: 2355-2363 [PMID:1535660]
ChEMBL Inhibitory activity against dopamine receptor D2 by 3H ligand binding experiments. B 6.2 pIC50 630 nM IC50 J. Med. Chem. (1991) 34: 616-624 [PMID:1995885]
ChEMBL In vitro antagonistic activity against Dopamine receptor D2 was evaluated for the inhibition of [3H]spiperone binding B 6.25 pIC50 565 nM IC50 J. Med. Chem. (1988) 31: 1548-1558 [PMID:3397992]
ChEMBL Binding affinity against dopamine D2 receptor in rat brain synaptic membrane using [3H]-spiperone as radioligand B 6.32 pIC50 480 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 619-624 [PMID:9871571]
ChEMBL Inhibition of [3H]- spiperone binding to rat brain Dopamine receptor D2 B 6.32 pIC50 480 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 1551-1554 [PMID:9873388]
ChEMBL Concentration of compound required to inhibit the binding of radioligand [3H]spiperone to Dopamine receptor D2 in rat brain synaptic membrane B 6.35 pIC50 444 nM IC50 J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 7.17 pKi 68 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells B 7.57 pKi 27 nM Ki J. Med. Chem. (2003) 46: 4377-4392 [PMID:14521403]
ChEMBL Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting. B 7.8 pKi 16 nM Ki US-9132134-B2. Methods for treating GI tract disorders (2015)
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.7 pIC50 200 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum B 7.21 pIC50 61.3 nM IC50 J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
Lactoperoxidase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2295561] [UniProtKB: P80025]
ChEMBL Inhibition of bovine milk LPO assessed as reduction in NaOSCN production in presence of H2O2/NaSCN after 5 mins B 5.3 pIC50 >5000 nM IC50 J Med Chem (2017) 60: 6563-6586 [PMID:28671460]
myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164]
ChEMBL Inhibition of recombinant MPO (unknown origin) assessed as reduction in LDL oxidation in presence of H2O2 and HCl after 5 mins by ELISA B 5.3 pIC50 >5000 nM IC50 J Med Chem (2017) 60: 6563-6586 [PMID:28671460]
ChEMBL Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins B 6.46 pIC50 350 nM IC50 J Med Chem (2017) 60: 6563-6586 [PMID:28671460]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity was evaluated by 5-hydroxytryptamine 1A receptor agonism in the pig cortex by displacing 8-OH-DPAT B 5.1 pKd 5.1 - pKD J. Med. Chem. (1995) 38: 2326-2330 [PMID:7608898]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.98 pKi 1050 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.43 pIC50 3675 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity was evaluated by 5-hydroxytryptamine 2A receptor agonism in the rat cortex by displacing ketanserin B 5.4 pKd 5.4 - pKD J. Med. Chem. (1995) 38: 2326-2330 [PMID:7608898]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.4 pKi 401 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.2 pIC50 630 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]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.9 pKi 1248 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.62 pIC50 2383 nM IC50 DrugMatrix in vitro pharmacology data
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
ChEMBL Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor of isolated guinea pig ileum (GPI) F 5.2 pKd 6309.57 nM Kd Bioorg. Med. Chem. Lett. (1992) 2: 461-466
ChEMBL Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated perfused rabbit heart (RH) F 7.1 pKd 79.43 nM Kd Bioorg. Med. Chem. Lett. (1992) 2: 461-466
ChEMBL Potency at neuronal 5-hydroxytryptamine 3 receptors in the rabbit heart B 7.3 pKd 50.12 nM Kd J. Med. Chem. (1990) 33: 1594-1600 [PMID:2342053]
ChEMBL Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated rabbit vagus nerve (RVN) F 7.3 pKd 50.12 nM Kd Bioorg. Med. Chem. Lett. (1992) 2: 461-466
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373374] [UniProtKB: P35563Q9JJ16]
ChEMBL Displacement of the 5-hydroxytryptamine 3 receptor ligand [3H]GR-65630 from rat brain cortical membranes. B 6 pKi 995 nM Ki J. Med. Chem. (1992) 35: 895-903 [PMID:1312602]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand B 6.3 pKi 502 nM Ki J. Med. Chem. (1990) 33: 3176-3181 [PMID:2258903]
ChEMBL pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor B 6.3 pKi 501.19 nM Ki J. Med. Chem. (1990) 33: 3176-3181 [PMID:2258903]
ChEMBL Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. B 6.31 pKi 490 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 263-266
ChEMBL Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 as radioligand in rat posterior cortex B 6.35 pKi 443 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 795-798
ChEMBL Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 in rat posterior cortex B 6.35 pKi 443 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 1433-1436
ChEMBL Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex B 6.46 pKi 348 nM Ki J. Med. Chem. (1998) 41: 311-317 [PMID:9464362]
ChEMBL Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor B 6.62 pKi 240 nM Ki J. Med. Chem. (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]quipazine as radioligand in rat cortex B 6.64 pKi 229.09 nM Ki J. Med. Chem. (1990) 33: 1594-1600 [PMID:2342053]
ChEMBL Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor B 6.68 pKi 210 nM Ki J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
ChEMBL Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex B 6.7 pKi 199.53 nM Ki J. Med. Chem. (1990) 33: 1594-1600 [PMID:2342053]
ChEMBL Tested for its binding affinity by measuring its ability to displace [3H]granisetron from 5-hydroxytryptamine 3 receptor in rat cortex B 6.8 pKi 158.49 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 633-634
ChEMBL Binding affinity against 5-hydroxytryptamine 3 receptor in rat cortical membrane using [3H]GR-65630 as radioligand B 6.06 pIC50 880 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 619-624 [PMID:9871571]
ChEMBL Inhibition of [3H]GR-65630 binding to rat cortical membrane 5-hydroxytryptamine 3 receptor B 6.06 pIC50 880 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 1551-1554 [PMID:9873388]
ChEMBL Concentration required to inhibit the binding of radioligand [3H]GR-65630 to serotonin 5-hydroxytryptamine-3 receptor (5-HT 3 receptor)in rat brain cortical membrane B 6.64 pIC50 228 nM IC50 J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae F 6.1 pEC50 794.33 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 2477-2480
5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
GtoPdb - - 6 pKi - - - FEBS Lett. (1996) 398: 19-25 [PMID:8946946]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand B 6 pKi >1000 nM Ki J. Med. Chem. (1997) 40: 608-621 [PMID:9046352]
ChEMBL Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum B 6.01 pKi 975 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 1433-1436
ChEMBL Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum B 6.01 pKi 974 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 795-798
ChEMBL Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement. B 6.05 pKi 900 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 263-266
ChEMBL In vitro relaxation of carbachol pre-contracted rat oesophageal TMM. F 5.72 pEC50 1920 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 263-266
ChEMBL Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae F 6.1 pEC50 794.33 nM EC50 Bioorg. Med. Chem. Lett. (1993) 3: 633-634
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor B 6.26 pKi 546 nM Ki J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
ChEMBL Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum B 6.04 pIC50 912 nM IC50 J. Med. Chem. (2003) 46: 702-715 [PMID:12593651]
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum F 8.24 pEC50 5.7 nM EC50 J. Med. Chem. (1997) 40: 608-621 [PMID:9046352]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.02 pIC50 94800 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 5.7 pKi - - - Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 6.45 pKi 354 nM Ki Neuropharmacology (2001) 41: 282-4 [PMID:11489465];
Br. J. Pharmacol. (1996) 118: 1237-45 [PMID:8818349]

ChEMBL data shown on this page come from version 27:

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]