ChEMBL ligand: CHEMBL225230
D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] 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] There should be some charts here, you may need to enable JavaScript!
L-Tyrosine hydroxylase /Tyrosine 3-hydroxylase in Human [ChEMBL: CHEMBL1969] [GtoPdb: 1243] [UniProtKB: P07101] 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
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells	B	5.74	pKd	1816	nM	Kd	J Med Chem (1996) 39: 850-859 [PMID:8632409]
ChEMBL	Affinity towards Dopamine receptor D1	B	5.82	pKi	1510	nM	Ki	J Med Chem (1998) 41: 4385-4399 [PMID:9784114]
ChEMBL	Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assay	B	6.31	pKi	490	nM	Ki	ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830]
ChEMBL	Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assay	B	9	pKi	1	nM	Ki	ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830]
ChEMBL	Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay	B	5.72	pEC50	1884	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
ChEMBL	Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay	B	5.73	pEC50	1862.09	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
ChEMBL	Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay	F	8.96	pEC50	1.1	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
ChEMBL	Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay	F	8.96	pEC50	1.1	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL	Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum	B	5.47	pKi	3410	nM	Ki	J Med Chem (2008) 51: 983-987 [PMID:18251489]
ChEMBL	Displacement of [3H]SCH-23390 from rat dopamine D1 receptor	B	6.14	pKi	730	nM	Ki	J Med Chem (2007) 50: 171-181 [PMID:17228858]
ChEMBL	Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390	B	6.47	pKi	340	nM	Ki	J Med Chem (1991) 34: 24-28 [PMID:1671415]
ChEMBL	Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand	B	6.47	pKi	340	nM	Ki	J Med Chem (1990) 33: 1800-1805 [PMID:1971309]
ChEMBL	Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane	B	6.19	pIC50	640	nM	IC50	J Med Chem (1990) 33: 3122-3124 [PMID:2147956]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Equilibrium dissociation constant against recombinant Dopamine receptor D2A expressed in COS7 cells	B	7.7	pKd	20	nM	Kd	J Med Chem (1996) 39: 850-859 [PMID:8632409]
ChEMBL	Affinity towards Dopamine receptor D2	B	7.3	pKi	50	nM	Ki	J Med Chem (1998) 41: 4385-4399 [PMID:9784114]
GtoPdb	-	-	8.9	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621]
ChEMBL	Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay	F	7.6	pEC50	25.12	nM	EC50	J Med Chem (2004) 47: 6595-6602 [PMID:15588094]
ChEMBL	Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay	B	8.93	pEC50	1.18	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
ChEMBL	Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay	B	8.93	pEC50	1.18	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
ChEMBL	Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay	F	10.4	pEC50	0.04	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
ChEMBL	Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay	F	10.4	pEC50	0.04	nM	EC50	ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974]
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	6.28	pKd	520	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	6.43	pKd	370	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	7.4	pKd	40	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	8.05	pKd	9	nM	Kd	J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D2 receptor low binding site in Sprague-Dawley rat striatum by scintillation counting	B	7.27	pKi	54	nM	Ki	ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830]
ChEMBL	Displacement of [3H]raclopride from rat dopamine D2 receptor	B	8	pKi	10	nM	Ki	J Med Chem (2007) 50: 171-181 [PMID:17228858]
ChEMBL	Displacement of [3H]neomonapride from dopamine D2 receptor in rat striatum	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2008) 51: 983-987 [PMID:18251489]
ChEMBL	Compound was evaluated for its ability to inhibit dopamine receptor D2 in rat striatum using [3H]-spiperone	B	9.1	pKi	0.8	nM	Ki	J Med Chem (1991) 34: 24-28 [PMID:1671415]
ChEMBL	Binding affinity at rat striatal Dopamine receptor D2 using [3H]- piperone radioligand	B	9.1	pKi	0.8	nM	Ki	J Med Chem (1990) 33: 1800-1805 [PMID:1971309]
ChEMBL	Displacement of [3H]domperidone from dopamine D2 receptor high binding site in Sprague-Dawley rat striatum by scintillation counting	B	9.74	pKi	0.18	nM	Ki	ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830]
ChEMBL	Evaluated for the affinity against Dopamine receptor D2 in rat striatal membranes	B	8	pIC50	10	nM	IC50	J Med Chem (1988) 31: 1466-1471 [PMID:2968456]
ChEMBL	Binding affinity against Dopamine receptor D2 from rat brain corpus striatum membrane	B	8.32	pIC50	4.8	nM	IC50	J Med Chem (1990) 33: 3122-3124 [PMID:2147956]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb	-	-	8.7	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621]
ChEMBL	Displacement of [3H]domperidone from human dopamine D3 receptor expressed in human HEK293 cells by scintillation counting	B	9.36	pKi	0.44	nM	Ki	ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830]
L-Tyrosine hydroxylase /Tyrosine 3-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1969] [GtoPdb: 1243] [UniProtKB: P07101]
ChEMBL	Inhibition of tyrosine hydroxylase	B	6.52	pIC50	300	nM	IC50	J Med Chem (2007) 50: 171-181 [PMID:17228858]

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]