ChEMBL ligand: CHEMBL444309
D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] There should be some charts here, you may need to enable JavaScript!
D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] 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/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of 3H-N-Methylspiperone from DRD2 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay	B	4.69	pKi	20579	nM	Ki	Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL	Displacement of 3H-N-Methylspiperone from DRD2 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay	B	4.75	pKi	17782.79	nM	Ki	Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL	Binding affinity to D2R (unknown origin) assessed as inhibition constant	B	4.77	pKi	>17000	nM	Ki	Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL	Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines	B	5.77	pKi	>1700	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Inhibition of human dopamine D2 receptor	B	5.77	pKi	>1700	nM	Ki	J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells	B	5.77	pKi	>1700	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells.	B	5.77	pKi	>1700	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Affinity to displace [3H]spiperone from cloned human Dopamine receptor D3 (hD3) stably expressed in HEK393 cell lines	B	6.11	pKi	770	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells	B	6.11	pKi	770	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells.	B	6.11	pKi	770	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Binding affinity to D3R (unknown origin) assessed as inhibition constant	B	6.11	pKi	770	nM	Ki	Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL	Inhibition of human dopamine D3 receptor	B	6.32	pKi	480	nM	Ki	J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Displacement of 3H-N-Methylspiperone from DRD4 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay	B	8.24	pKi	5.82	nM	Ki	Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL	Displacement of 3H-N-Methylspiperone from DRD4 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay	B	8.28	pKi	5.25	nM	Ki	Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells	B	8.46	pKi	3.5	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.	B	8.46	pKi	3.5	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant	B	8.46	pKi	3.5	nM	Ki	Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL	Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines	B	8.46	pKi	3.5	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Binding affinity towards human dopamine receptor D4	B	8.46	pKi	3.5	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
GtoPdb	-	-	8.5	pKi	3.16	nM	Ki	J Med Chem (1996) 39: 1943-5 [PMID:8642551]
ChEMBL	Inhibition of human dopamine D4 receptor	B	8.6	pKi	2.5	nM	Ki	J Med Chem (2017) 60: 7233-7243 [PMID:28489950]

ChEMBL data shown on this page come from version 36:

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]