ChEMBL ligand: CHEMBL285755
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/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] There should be some charts here, you may need to enable JavaScript!
D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] 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!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] 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
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]spiperone from cloned dopamine D2L receptor expressed in HEK cells	B	6.69	pKi	202	nM	Ki	J Med Chem (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter	B	6.84	pKi	143	nM	Ki	J Med Chem (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL	Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D2 in Sf 9 cells	B	6.85	pKi	142	nM	Ki	J Med Chem (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL	Tested for the inhibitory activity against D2H (high-affinity states) receptor in infected HEK 293 cells.	B	6.85	pKi	142	nM	Ki	J Med Chem (1994) 37: 4245-4250 [PMID:7990123]
GtoPdb	-	-	7.6	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]
ChEMBL	Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter	B	8.64	pKi	2.27	nM	Ki	J Med Chem (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL	Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	F	7.4	pEC50	39.8	nM	EC50	J Med Chem (2008) 51: 3005-3019 [PMID:18410082]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
GtoPdb	-	-	6.2	pKi	-	-	-	J Med Chem (1994) 37: 4245-50 [PMID:7990123]
ChEMBL	Displacement of [3H]Spiperone from rat dopamine D2L receptor expressed in HEK293 cells	B	6.51	pKi	311	nM	Ki	J Med Chem (2008) 51: 7806-7819 [PMID:19053758]
ChEMBL	Displacement of [3H]spiperone from rat D2 receptor expressed in HEK293 cells	B	6.51	pKi	311	nM	Ki	Bioorg Med Chem (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL	Displacement of [3H]spiperone from rat dopamine D2L receptor expressed in HEK293 cells	B	6.51	pKi	311	nM	Ki	Bioorg Med Chem (2009) 17: 3923-3933 [PMID:19427222]
ChEMBL	Displacement of [3H]spiperone from rat dopamine D2L receptor expressed in HEK293 cells	B	6.69	pKi	202	nM	Ki	J Med Chem (2008) 51: 3005-3019 [PMID:18410082]
ChEMBL	Tested for inhibition of the binding of [125I]NCQ298 to D2 receptor	B	6.85	pKi	142	nM	Ki	J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL	Binding affinity against dopamine receptor D2 in rat brain tissue using [3H]spiperone	B	7.27	pKi	54	nM	Ki	J Med Chem (1993) 36: 3409-3416 [PMID:8230131]
ChEMBL	Displacement of the radioligand [3H]spiperone from D2 receptor	B	7.27	pKi	54	nM	Ki	J Med Chem (1994) 37: 3263-3273 [PMID:7932553]
ChEMBL	Tested in vitro for the inhibition of [3H]raclopride binding to Dopamine receptor D2 in rat striatum	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem Lett (1997) 7: 2759-2764
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	6.72	pIC50	192	nM	IC50	Med Chem Res (2004) 13: 25-33
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	6.74	pIC50	180	nM	IC50	Med Chem Res (2004) 13: 25-33
ChEMBL	Potency to displace the specific in vitro binding of [3H]DP-5,6-ADTN to rat striatal membrane	B	7.52	pIC50	30	nM	IC50	J Med Chem (1988) 31: 2178-2182 [PMID:2903247]
ChEMBL	Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min	F	8.73	pEC50	1.88	nM	EC50	Med Chem Res (2004) 13: 25-33
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 D3.32E mutant receptor expressed in human HEK293 cells	B	5.85	pKi	1400	nM	Ki	J Med Chem (2008) 51: 6829-6838 [PMID:18834111]
ChEMBL	Displacement of [3H]spiperone from human D3 F6.51W mutant receptor expressed in human HEK293 cells	B	6.57	pKi	270	nM	Ki	J Med Chem (2008) 51: 6829-6838 [PMID:18834111]
GtoPdb	-	-	8.4	pKi	3.98	nM	Ki	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621]; Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; J Med Chem (1994) 37: 4245-50 [PMID:7990123]
ChEMBL	Displacement of [3H]spiperone from human wild type D3 receptor expressed in human HEK293 cells	B	8.44	pKi	3.6	nM	Ki	J Med Chem (2008) 51: 6829-6838 [PMID:18834111]
ChEMBL	Tested for the inhibitory activity against Dopamine D3 receptor in infected Sf9 cells	B	8.54	pKi	2.9	nM	Ki	J Med Chem (1994) 37: 4245-4250 [PMID:7990123]
ChEMBL	Displacement of [3H]spiperone from cloned dopamine D3 receptor expressed in HEK cells	B	8.63	pKi	2.35	nM	Ki	J Med Chem (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL	Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter	B	8.76	pKi	1.75	nM	Ki	J Med Chem (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL	Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter	B	8.83	pKi	1.49	nM	Ki	J Med Chem (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL	Tested in vitro for the inhibition of [3H]U-86170 binding to Dopamine receptor D3, expressed in cloned CHO cells	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem Lett (1997) 7: 2759-2764
ChEMBL	Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding	F	9.27	pEC50	0.53	nM	EC50	J Med Chem (2008) 51: 3005-3019 [PMID:18410082]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL	Tested for binding affinity against dopamine receptor D3	B	9.17	pKd	0.67	nM	Kd	J Med Chem (1993) 36: 4308-4312 [PMID:8277513]
ChEMBL	Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells	B	8.21	pKi	6.19	nM	Ki	Bioorg Med Chem (2009) 17: 3923-3933 [PMID:19427222]
ChEMBL	Displacement of [3H]spiperone from rat D3 receptor expressed in HEK293 cells	B	8.21	pKi	6.19	nM	Ki	Bioorg Med Chem (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL	Displacement of [3H]Spiperone from rat dopamine D3 receptor expressed in HEK293 cells	B	8.21	pKi	6.19	nM	Ki	J Med Chem (2008) 51: 7806-7819 [PMID:19053758]
ChEMBL	Tested for inhibition of the binding of [125I]NCQ298 to dopamine receptor D3	B	8.54	pKi	2.9	nM	Ki	J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL	Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D3 in Sf 9 cells	B	8.54	pKi	2.9	nM	Ki	J Med Chem (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL	Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells	B	8.63	pKi	2.35	nM	Ki	J Med Chem (2008) 51: 3005-3019 [PMID:18410082]
ChEMBL	Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.	B	8.93	pKi	1.18	nM	Ki	J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	8.9	pIC50	1.25	nM	IC50	Med Chem Res (2004) 13: 25-33
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	8.95	pIC50	1.11	nM	IC50	Med Chem Res (2004) 13: 25-33
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells	B	6.83	pKi	148	nM	Ki	Bioorg Med Chem Lett (1997) 7: 2759-2764
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Tested in vitro for the inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor, expressed in cloned CHO cells.	B	7.33	pKi	47	nM	Ki	Bioorg Med Chem Lett (1997) 7: 2759-2764
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Displacement of the radioligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor	B	5.55	pKi	2810	nM	Ki	J Med Chem (1994) 37: 3263-3273 [PMID:7932553]
ChEMBL	Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand	B	5.55	pKi	2800	nM	Ki	J Med Chem (1993) 36: 3409-3416 [PMID:8230131]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain	B	7.14	pKi	72.7	nM	Ki	J Med Chem (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL	Tested for the inhibitory activity against 5-hydroxytryptamine 1A receptor in rat hippocampal	B	7.14	pKi	72.7	nM	Ki	J Med Chem (1994) 37: 4245-4250 [PMID:7990123]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL	Tested for the inhibitory activity against sigma receptor rat cerebellar	B	7.63	pKi	23.2	nM	Ki	J Med Chem (1994) 37: 4245-4250 [PMID:7990123]

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]