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]
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]
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]
GtoPdb	-	-	9.6	pKd	0.27	nM	Kd	J Neuroimmunol (1995) 58: 139-44 [PMID:7759603]
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]
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]
GtoPdb	-	-	9.1	pKd	0.79	nM	Kd	Proc Natl Acad Sci USA (1992) 89: 8155-9 [PMID:1518841]
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 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]