ChEMBL ligand: CHEMBL1112 (Abilify, Abilify maintena, Abilify maintena kit, Abilify mycite, Abilify mycite kit, Aripiprazol, Aripiprazole, Aripiprazole mylan pharma (previously aripiprazole pharmathen), Aripiprex, NSC-759266, OPC-14597, OPC-31)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] There should be some charts here, you may need to enable JavaScript!
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] There should be some charts here, you may need to enable JavaScript!
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] There should be some charts here, you may need to enable JavaScript!
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] There should be some charts here, you may need to enable JavaScript!
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] There should be some charts here, you may need to enable JavaScript!
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] 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] D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] There should be some charts here, you may need to enable JavaScript!
D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389] There should be some charts here, you may need to enable JavaScript!
H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] There should be some charts here, you may need to enable JavaScript!
M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] There should be some charts here, you may need to enable JavaScript!
M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] There should be some charts here, you may need to enable JavaScript!
M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] There should be some charts here, you may need to enable JavaScript!
M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] There should be some charts here, you may need to enable JavaScript!
M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] 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!
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] There should be some charts here, you may need to enable JavaScript!
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] There should be some charts here, you may need to enable JavaScript!
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] There should be some charts here, you may need to enable JavaScript!
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] There should be some charts here, you may need to enable JavaScript!
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] There should be some charts here, you may need to enable JavaScript!
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] There should be some charts here, you may need to enable JavaScript!
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] 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
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.59	pKi	26	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay	B	6.77	pIC50	170	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay	F	6.77	pIC50	170	nM	IC50	Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL	Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	F	6.77	pIC50	170	nM	IC50	Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL	Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL	Binding affinity to adrenergic alpha2B receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL	Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]-clonidine from human alpha 2C receptor incubated for 1 hr by liquid scintillation counting method	B	7.42	pKi	37.9	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	5.94	pKi	1148.15	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	5.94	pKi	1146	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	6.05	pKi	895	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis	B	6.51	pKi	310	nM	Ki	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay	B	6.51	pKi	310	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes	B	6.51	pKi	310	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay	B	6.51	pKi	310	nM	Ki	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	5.71	pKi	1960	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]N-methylspiperone from Dopamine D2 receptor (unknown origin) expressed in HEK293T cell membrane incubated for 2 hrs by radioligand competitive binding based MicroBeta TriLux reader method	B	5.66	pKi	2180	nM	Ki	J Med Chem (2023) 66: 6274-6287 [PMID:37130037]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin)	B	8.01	pKi	9.7	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	8.1	pKi	8	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method	B	8.35	pKi	4.5	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Displacement of [3H]-Spiperone from human dopamine D2L receptor expressed in CHO cells	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5666-5669 [PMID:20801650]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2L receptor expressed in CHO cells after 1.5 hrs by microbeta counting method	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2012) 55: 7141-7153 [PMID:22845053]
ChEMBL	Displacement of [3H]-N-methylspiperone from human D2 receptor incubated for 1 hr by liquid scintillation counting method	B	8.48	pKi	3.3	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D2 receptor incubated for 1 hr by liquid scintillation counting method	B	8.48	pKi	3.3	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2 receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	8.48	pKi	3.3	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [3H]methylspiperone from human D2 receptor by radio ligand binding assay	B	8.48	pKi	3.3	nM	Ki	Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting	B	8.48	pKi	3.3	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Displacement of [125I]ABN from human recombinant D2L receptor expressed in HEK cells after 60 mins by gamma counter	B	8.51	pKi	3.1	nM	Ki	Bioorg Med Chem (2011) 19: 3502-3511 [PMID:21536445]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells	B	8.55	pKi	2.8	nM	Ki	J Med Chem (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells	B	8.59	pKi	2.6	nM	Ki	J Med Chem (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL	Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.67	pKi	2.14	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.67	pKi	2.13	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Binding affinity to dopamine D2	B	8.74	pKi	1.82	nM	Ki	J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D2L receptor expressed in CHO cells	B	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2621-2625 [PMID:21353774]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	8.8	pKi	1.6	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay	B	9	pKi	<1	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	9.1	pKi	0.8	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Displacement of [3H]-raclopride from human dopamine D2L receptor expressed in HEK293 after 1 hr	B	9.1	pKi	0.8	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin)	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
GtoPdb	-	-	9.1	pKi	0.8	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293 cell membranes measured after 60 mins by MicroBeta scintillation counting method	B	9.16	pKi	0.69	nM	Ki	J Med Chem (2021) 64: 15313-15333 [PMID:34636551]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay	B	9.27	pKi	0.54	nM	Ki	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Displacement of [3H]spiperone from human Dopamine D2L receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis	B	9.28	pKi	0.53	nM	Ki	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Displacement of [3H]spiperone from human D2LR expressed in CHO cell membranes	B	9.28	pKi	0.52	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Displacement of [3H]spiperone from human D2LR expressed in CHO cell membranes by radioligand binding assay	B	9.28	pKi	0.52	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cell membranes by radioligand competition binding assay	B	9.32	pKi	0.48	nM	Ki	Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL	Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis	B	9.32	pKi	0.48	nM	Ki	J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL	Displacement of [3H]spiperone from human Dopamine D2S receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis	B	9.35	pKi	0.45	nM	Ki	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay	B	9.35	pKi	0.45	nM	Ki	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Displacement of [3H]spiperone from human D2SR expressed in CHO cell membranes by radioligand binding assay	B	9.42	pKi	0.38	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]spiperone from human D2SR expressed in CHO cell membranes	B	9.42	pKi	0.38	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells	B	9.46	pKi	0.34	nM	Ki	J Med Chem (2015) 58: 5361-5380 [PMID:25826710]
ChEMBL	Partial agonist activity at human D2 receptor assessed as inhibition constant	B	9.47	pKi	0.34	nM	Ki	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method	B	9.47	pKi	0.34	nM	Ki	Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL	Modulation of human D2L receptor	B	9.52	pKi	0.3	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Displacement of [3H]raclopride from human D2 dopamine receptor expressed in CHO cell membranes	B	9.7	pKi	0.2	nM	Ki	Bioorg Med Chem Lett (2013) 23: 543-547 [PMID:23237836]
ChEMBL	Partial agonist activity at human D2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis	B	7.42	pIC50	38.02	nM	IC50	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Antagonistic activity at human dopamine D2 receptor measured after 60 mins by Lance Ultra cAMP assay	F	7.49	pIC50	32	nM	IC50	Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL	Antagonistic activity at human dopamine D2 receptor measured after 60 mins by Ultra Lance cAMP assay	F	7.76	pIC50	17.2	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	B	7.95	pIC50	11.22	nM	IC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	B	7.96	pIC50	11	nM	IC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay	F	8.12	pIC50	7.6	nM	IC50	Bioorg Med Chem Lett (2013) 23: 543-547 [PMID:23237836]
ChEMBL	Partial agonist activity at human D2 receptor expressed in HEK293T cells assessed as beta-arrestin recruitment preincubated for 10 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay	B	9	pIC50	1	nM	IC50	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay	B	5.3	pEC50	>5000	nM	EC50	J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay	F	5.3	pEC50	>5000	nM	EC50	J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL	Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay	B	5.3	pEC50	>5000	nM	EC50	J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay	B	5.3	pEC50	>5000	nM	EC50	J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	B	5.96	pEC50	1100	nM	EC50	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	B	6.13	pEC50	740	nM	EC50	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay	F	6.8	pEC50	160	nM	EC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	F	6.8	pEC50	160	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	F	6.8	pEC50	158.49	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay	F	6.8	pEC50	158.49	nM	EC50	Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL	Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay	F	6.8	pEC50	158.49	nM	EC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay	F	6.89	pEC50	130	nM	EC50	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	F	7.41	pEC50	39	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay	F	7.41	pEC50	38.9	nM	EC50	Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	F	7.41	pEC50	38.9	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
GtoPdb	Measuring cAMP production via the Gi-coupled signaling pathway	-	7.42	pEC50	38	nM	EC50	Proc Natl Acad Sci USA (2011) 108: 18488-93 [PMID:22025698]
ChEMBL	Partial agonist activity at human D2 receptor assessed as increase in cAMP accumulation	B	7.42	pEC50	38	nM	EC50	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay	B	7.71	pEC50	19.4	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay	F	7.72	pEC50	19.05	nM	EC50	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay	F	7.72	pEC50	18.9	nM	EC50	J Med Chem (2023) 66: 6274-6287 [PMID:37130037]
ChEMBL	Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay	F	7.72	pEC50	18.9	nM	EC50	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay	B	7.76	pEC50	17.5	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay	B	7.83	pEC50	14.9	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay	F	7.91	pEC50	12.4	nM	EC50	J Med Chem (2023) 66: 6274-6287 [PMID:37130037]
ChEMBL	Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay	F	7.91	pEC50	12.4	nM	EC50	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay	F	7.91	pEC50	12.3	nM	EC50	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay	B	8.06	pEC50	8.7	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay	B	8.32	pEC50	4.8	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay	F	8.4	pEC50	4	nM	EC50	J Med Chem (2012) 55: 7141-7153 [PMID:22845053]
ChEMBL	Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitment	B	8.4	pEC50	4	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL	Partial agonist activity at human D2 receptor assessed as beta arrestin-2 recruitment	B	8.62	pEC50	2.4	nM	EC50	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay	F	9	pEC50	1	nM	EC50	J Med Chem (2012) 55: 7141-7153 [PMID:22845053]
ChEMBL	Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay	F	9	pEC50	1	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL	Displacement of [3H]spiperone from D2 receptor in rat striatum measured after 15 mins by liquid scintillation counting method	B	8.01	pKi	9.7	nM	Ki	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
GtoPdb	-	-	9.7	pKi	-	-	-	Mol Pharmacol (2000) 57: 144-52 [PMID:10617689]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	7.72	pKi	19	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin)	B	7.97	pKi	10.8	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting	B	8.01	pKi	9.7	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Displacement of [3H]-methylspiperone from human dopamine D3 receptor expressed in HEK293 after 1 hr	B	8.01	pKi	9.7	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D3 receptor incubated for 1 hr by liquid scintillation counting method	B	8.01	pKi	9.7	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]-N-methylspiperone from human D3 receptor incubated for 1 hr by liquid scintillation counting method	B	8.01	pKi	9.7	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
ChEMBL	Displacement of [3H]N-methylspiperone from human D3 receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	8.01	pKi	9.7	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [125I]ABN from human recombinant D3 receptor expressed in HEK cells after 60 mins by gamma counter	B	8.17	pKi	6.8	nM	Ki	Bioorg Med Chem (2011) 19: 3502-3511 [PMID:21536445]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane	B	8.35	pKi	4.47	nM	Ki	J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL	Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.4	pKi	4.02	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	8.4	pKi	3.98	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.4	pKi	3.98	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis	B	8.45	pKi	3.57	nM	Ki	J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin)	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assay	B	8.52	pKi	3	nM	Ki	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Displacement of [3H]spiperone from human D3R expressed in CHO cell membranes by radioligand binding assay	B	8.54	pKi	2.9	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]spiperone from human D3R expressed in CHO cell membranes	B	8.54	pKi	2.9	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by MicroBeta scintillation counting method	B	8.63	pKi	2.34	nM	Ki	J Med Chem (2021) 64: 15313-15333 [PMID:34636551]
ChEMBL	Displacement of [3H]spiperone from human Dopamine D3 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis	B	8.64	pKi	2.3	nM	Ki	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells	B	9	pKi	1	nM	Ki	J Med Chem (2015) 58: 5361-5380 [PMID:25826710]
ChEMBL	Partial agonist activity at human D3 receptor assessed as inhibition constant	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Partial agonist activity at human D3 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis	B	7.09	pIC50	81.28	nM	IC50	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay	F	7.7	pEC50	20	nM	EC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	F	7.7	pEC50	20	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay	F	7.71	pEC50	19.5	nM	EC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	F	7.71	pEC50	19.5	nM	EC50	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL	Receptor Assay: Competitive binding test for receptors: 20 μl of each of the test compounds and 20 μl of the radioactive ligand together with 160 μl of the receptor proteins were added into the reaction tubes, and the final concentrations of the test compound and the positive drug were all 10 μmol/L. After 50 min of incubation in 30° C. water bath, the tubes were immediately moved to ice bath to terminate the reactions. GF/C glass fiber filter papers were used for rapid sucking filtration on a Millipore cell sample collector, elution buffer (50 mM Tris-HCl, PH 7.4) was applied for 3 ml×3 times, and microwave was applied for 4-5 min for drying. The filter papers were moved into 0.5 ml centrifuge tubes, and 500 μl of lipid-soluble scintillation solution was added. The tubes were allowed to stand still for over 30 min in dark, and the intensities of radioactivity were measured by a counter.	B	7.42	pIC50	37.9	nM	IC50	US-9018213-B2. Alicyclic[c] benzopyrone derivatives and uses thereof (2015)
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method	B	6.29	pKi	510	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting	B	6.29	pKi	510	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	6.6	pKi	251	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter	B	6.77	pKi	168	nM	Ki	Bioorg Med Chem (2011) 19: 3502-3511 [PMID:21536445]
ChEMBL	Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7	pKi	100.8	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7	pKi	100	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay	B	7.09	pKi	81	nM	Ki	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis	B	7.09	pKi	81	nM	Ki	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes	B	7.2	pKi	63	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay	B	7.2	pKi	63	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane	B	7.24	pKi	57.54	nM	Ki	J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells	B	7.24	pKi	57.1	nM	Ki	J Med Chem (2015) 58: 5361-5380 [PMID:25826710]
ChEMBL	Partial agonist activity at human D4 receptor assessed as inhibition constant	B	7.36	pKi	44	nM	Ki	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
ChEMBL	Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis	B	5.93	pIC50	1174.9	nM	IC50	J Med Chem (2021) 64: 8710-8726 [PMID:34110150]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL	Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	6.29	pKi	510	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
GtoPdb	-	-	7.3	pKi	-	-	-	Mol Pharmacol (2000) 57: 144-52 [PMID:10617689]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL	Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay	B	5.8	pKi	1600	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes	B	5.8	pKi	1600	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	5.98	pKi	1051	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method	B	5.99	pKi	1020	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Binding affinity to human ERG expressed in HEK293 cells	B	5.99	pKi	1020	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Displacement of [3H]dofetilide from human ERG	B	6.22	pKi	598	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5666-5669 [PMID:20801650]
ChEMBL	Inhibition of human ERG after 10 mins	B	5.41	pIC50	3860	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Inhibition of human ERG by auomated patch clamp assay	B	5.41	pIC50	3860	nM	IC50	Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
ChEMBL	Inhibition of human ERG	B	6	pIC50	<1000	nM	IC50	Bioorg Med Chem Lett (2010) 20: 7312-7316 [PMID:21055935]
ChEMBL	Inhibition of human ERG by automated patch method relative to control	B	6.05	pIC50	896.5	nM	IC50	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells by whole-cell patch clamp method	B	6.05	pIC50	896	nM	IC50	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Inhibition of human ERG	B	6.2	pIC50	630.96	nM	IC50	Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL	Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity to H1 histamine receptor (unknown origin)	B	7.21	pKi	61	nM	Ki	Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775]
GtoPdb	-	-	7.5	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.55	pKi	28	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	7.6	pKi	25.1	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting method	B	7.6	pKi	25.1	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
ChEMBL	Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay	B	6.38	pIC50	420	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	F	6.38	pIC50	420	nM	IC50	Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	F	6.38	pIC50	420	nM	IC50	Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL	Displacement of [3H]mepyramine from H1R in rat brain	B	5.52	pIC50	>3000	nM	IC50	Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL	Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL	Binding affinity to histamine H3 receptor (unknown origin)	B	5.63	pKi	2361	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL	Binding affinity to M1 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL	Binding affinity to M2 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL	Binding affinity to M3 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Antagonist activity at M3 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	F	4	pIC50	>100000	nM	IC50	Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL	Binding affinity to M4 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL	Binding affinity to M5 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL	Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis	B	6.11	pIC50	780	nM	IC50	J Med Chem (2011) 54: 1740-1751 [PMID:21341745]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	7.52	pKi	30	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity to 5-HT1A receptor (unknown origin)	B	7.7	pKi	19.8	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	7.74	pKi	18	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.88	pKi	13.3	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.88	pKi	13.18	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells	B	7.99	pKi	10.3	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2621-2625 [PMID:21353774]
ChEMBL	Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells	B	8.15	pKi	7	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5666-5669 [PMID:20801650]
GtoPdb	-	-	8.2	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 1400-11 [PMID:12784105]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method	B	8.25	pKi	5.6	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 after 1 hr	B	8.25	pKi	5.6	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Binding affinity to 5HT1A receptor (unknown origin)	B	8.25	pKi	5.6	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	8.25	pKi	5.6	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor by radio ligand binding assay	B	8.25	pKi	5.6	nM	Ki	Bioorg Med Chem Lett (2019) 29: 126667-126667 [PMID:31547945]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor by liquid scintillation counting	B	8.25	pKi	5.6	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor incubated for 1 hr by liquid scintillation counting method	B	8.25	pKi	5.6	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor incubated for 1 hr by liquid scintillation counting method	B	8.25	pKi	5.6	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	8.77	pKi	1.7	nM	Ki	Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL	pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).	B	6.35	pEC50	450	nM	EC50	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay	F	6.55	pEC50	285	nM	EC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay	F	7.62	pEC50	24	nM	EC50	Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Displacement of [3H](+)8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 30 mins by liquid scintillation counting method	B	7.7	pKi	19.8	nM	Ki	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry	B	8.25	pKi	5.6	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A receptor in rat CRL:CD(SD)BR-COBS hippocampus by scintillation spectrometry	B	8.25	pKi	5.6	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate	B	9.4	pKi	0.4	nM	Ki	Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652]
ChEMBL	Receptor Binding Assay: Isotope ligand 3H-8-OH-DPAT (67.0 Ci/mmol) was purchased from PerkinElmer Company; 5-HT was purchased from RBI Company; GF/C glass fiber filter paper was purchased from Whatman Company; Tris was imported and divided into aliquots; PPO, POPOP were purchased from Shanghai No. 1 Reagent Factory; lipid-soluble scintillation solution. Beckman LS-6500 Multi-function Liquid Scintillation Counter was used.Procedures(1) The prepared membrane was first applied with appropriate amount of buffer (0.05 M Tris-HCl buffer, containing 0.1% ascorbic acid, 10 um pargyline and 4 mM CaCl2), and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer (0.05 M Tris-HCl buffer, containing 0.1% ascorbic acid, 10 um pargyline and 4 mM CaCl2) were added into each reaction tube.	B	8.47	pIC50	3.35	nM	IC50	US-8993575-B2. [1,3,4] oxadiazole derivative and application thereof (2015)
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL	Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.1	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 1400-11 [PMID:12784105]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL	Binding affinity to serotonin 5-HT1D receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	7.2	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 1400-11 [PMID:12784105]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL	Binding affinity to serotonin 5-HT1E receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method	B	7.2	pKi	63	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	7.4	pKi	40	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [3H]-LSD from 5HT2A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.4	pKi	39.81	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-LSD from 5HT2A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.4	pKi	39.6	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells measured after 1.5 hrs by Microbeta plate reader method	B	7.55	pKi	28	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Displacement of [3H]-ketanserin from human 5HT2A receptor expressed in HEK293 after 1.5 hrs	B	7.68	pKi	21	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Displacement of [3H]-Ketanserin from 5-HT2A receptor (unknown origin) assessed as inhibition constant by radioligand binding assay	B	7.68	pKi	21	nM	Ki	J Med Chem (2024) 67: 1580-1610 [PMID:38190615]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells	B	7.8	pKi	15.85	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity to 5-HT2A receptor (unknown origin)	B	7.92	pKi	12.1	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL	Binding affinity to serotonin 5-HT2A receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity to human 5HT2A receptor	B	8.02	pKi	9.6	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2621-2625 [PMID:21353774]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	8.05	pKi	9	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [3H]-ketanserin from human 5HT2A receptor by liquid scintillation counting	B	8.06	pKi	8.7	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2A receptor incubated for 1 hr by liquid scintillation counting method	B	8.06	pKi	8.7	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
ChEMBL	Binding affinity to 5-HT2A receptor (unknown origin)	B	8.06	pKi	8.7	nM	Ki	Bioorg Med Chem Lett (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL	Displacement of [3H]-Ketanserin from human 5-HT2A receptor incubated for 1 hr by liquid scintillation counting method	B	8.06	pKi	8.7	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]Ketanserin from human 5-HT2A receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	8.06	pKi	8.7	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Binding affinity to 5HT2A receptor (unknown origin)	B	8.06	pKi	8.7	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
GtoPdb	-	-	8.1	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 1400-11 [PMID:12784105]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL	Binding affinity to human 5HT2A receptor	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5666-5669 [PMID:20801650]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293 cell membranes by radioligand competition binding assay	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL	Displacement of [3H]-ketanserin from human 5HT2A receptor expressed in HEK293 cells by competitive binding assay	B	8.4	pKi	4	nM	Ki	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2AR expressed in HEK293T cell membranes1	B	8.44	pKi	3.6	nM	Ki	Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2AR expressed in HEK293T cell membranes by radioligand binding assay	B	8.44	pKi	3.6	nM	Ki	J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL	Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in rat cortex tissue incubated for 30 mins by liquid scintillation counting method	B	8.47	pKi	3.4	nM	Ki	Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL	Binding affinity to 5-HT2A	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2011) 54: 6305-6318 [PMID:21823597]
ChEMBL	Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay	F	5.55	pIC50	2790	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay	F	5.96	pIC50	1100	nM	IC50	Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb	-	-	7.7	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 1400-11 [PMID:12784105]
ChEMBL	Displacement of [3H]ketanserin from rat cerebral cortex 5HT2A receptor measured after 15 mins by liquid scintillation counting method	B	7.92	pKi	12.1	nM	Ki	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry	B	8.06	pKi	8.7	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry	B	8.06	pKi	8.7	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate	B	8.15	pKi	7	nM	Ki	Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652]
ChEMBL	Receptor Binding Assay: Materials for the Receptor Binding AssayIsotope ligand [3H]-Ketanserin (67.0 Ci/mmol) was purchased from PerkinElmer Company; Methysergide was purchased from RBI Company; GF/C glass fiber filter paper was purchased from Whatman Company; Tris was imported and divided into aliquots; PPO, POPOP were purchased from Shanghai No. 1 Reagent Factory; lipid-soluble scintillation solution. Beckman LS-6500 Multi-function Liquid Scintillation Counter was used.Procedures(1) The prepared membrane was first applied with appropriate amount of buffer (0.05 M Tris-HCl buffer: 6.05 g of Tris was dissolved in 1000 ml of double-distilled water, and concentrated HCl was used to adjust to pH 7.5), and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer.	B	7.94	pIC50	11.51	nM	IC50	US-8993575-B2. [1,3,4] oxadiazole derivative and application thereof (2015)
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method	B	8.25	pKi	5.6	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	8.85	pKi	1.4	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells	B	8.9	pKi	1.26	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	9.44	pKi	0.36	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [3H]-LSD from human 5-HT2B receptor assessed as inhibition constant	B	9.44	pKi	0.36	nM	Ki	J Med Chem (2023) 66: 11027-11039 [PMID:37584406]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Binding affinity to serotonin 5-HT2C receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.	B	6.6	pKi	250	nM	Ki	US-9156822-B2. Functionally selective ligands of dopamine D2 receptors (2015)
ChEMBL	Displacement of [3H]-Mesulergine from human 5-HT2C receptor incubated for 1 hr by liquid scintillation counting method	B	6.74	pKi	180	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]-mesulergine from human 5HT2C receptor by liquid scintillation counting	B	6.74	pKi	180	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6.89	pKi	130	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.02	pKi	95.5	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.02	pKi	95.4	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells	B	7.3	pKi	50.12	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb	-	-	7.6	pKi	-	-	-	Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL	Binding affinity to 5HT2C receptor (unknown origin)	B	7.66	pKi	22	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells	B	7.66	pKi	22	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL	Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay	B	5.86	pIC50	1380	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3141-3147 [PMID:27173799]
ChEMBL	Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay	F	5.86	pIC50	1380	nM	IC50	Bioorg Med Chem Lett (2018) 28: 606-611 [PMID:29395980]
ChEMBL	Antagonist activity at 5-HT2C receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	F	5.86	pIC50	1380	nM	IC50	Eur J Med Chem (2018) 145: 74-85 [PMID:29324345]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL	Displacement of [3H]Mesulergine from rat 5-HT2C receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	7.12	pKi	76	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Receptor Binding Assay: (1) The prepared membrane was first applied with appropriate amount of homogenized liquid, and homogenizer was used for evenly dispersing. 15 tubes were mixed into a 100 ml container, and appropriate amount of homogenized liquid was added to give 50 ml of membrane suspension, which was reserved for future use.(2) 100 uL of membrane preparation and 100 uL of buffer were added into each reaction tube.(3) 100 uL of homogenized liquid was added into the total binding tube (TB), 100 uL of mianserin (final concentration 10-5 M) was added into the non-specific binding tube (NB), and 100 uL of the test compound (final concentration 10-5 M) was added into the specific binding tube (SB) for each compound.(4) 10 uL of radioactive ligand [3H]-mesulergine was respectively added into each reaction tube (2 parallel tubes were used for each reaction tube, and each of them was placed on ice when adding sample).(5) Each of the reaction tubes was incubated at 37 degree.	B	7.59	pIC50	25.7	nM	IC50	US-9018213-B2. Alicyclic[c] benzopyrone derivatives and uses thereof (2015)
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: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL	Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells	B	6.3	pKi	501.19	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL	Binding affinity to serotonin 5-HT3 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL	Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL	Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells	B	6.24	pKi	574	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL	Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method	B	6.5	pKi	318	nM	Ki	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Binding affinity to 5-HT6 receptor (unknown origin)	B	6.5	pKi	318	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127909-127909 [PMID:33705900]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells	B	6.7	pKi	199.53	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr	B	7.05	pKi	90	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	7.05	pKi	89	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb	-	-	6.8	pKi	-	-	-	Neuropsychopharmacology (1999) 20: 612-27 [PMID:10327430]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	B	7.2	pKi	63.1	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	7.36	pKi	44	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 after 1 hr	B	7.59	pKi	26	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 7 receptor	B	7.85	pKi	14	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting	B	7.99	pKi	10.3	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting	B	7.99	pKi	10.3	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method	B	7.99	pKi	10.3	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method	B	8	pKi	10	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL	Displacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting method	B	7.05	pKi	89.4	nM	Ki	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
GtoPdb	-	-	7.8	pKi	-	-	-	Neuropsychopharmacology (1999) 20: 612-27 [PMID:10327430]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Displacement of [3H]Citalopram from human SERT expressed in cell membranes after 1 hr by liquid scintillation counting	B	5.97	pKi	1080	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Displacement of [3H]-citalopram from human SERT by liquid scintillation counting	B	5.97	pKi	1080	nM	Ki	Bioorg Med Chem (2021) 30: 115943-115943 [PMID:33338898]
ChEMBL	Displacement of [3H]-citalopram from human SERT receptor incubated for 1 hr by liquid scintillation counting method	B	5.97	pKi	1080	nM	Ki	Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6.62	pKi	240	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Binding affinity to SERT	B	7.01	pKi	98	nM	Ki	J Med Chem (2011) 54: 6305-6318 [PMID:21823597]
ChEMBL	Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells	B	7.5	pKi	31.62	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Displacement of [3H]-citalopram from SERT in rat cerebral cortex after 1 hr by scintillation counting	B	5.97	pKi	1080	nM	Ki	Eur J Med Chem (2013) 60: 42-50 [PMID:23279866]

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]