ChEMBL ligand: CHEMBL42 (Clozapina, Clozapine, Clozapine (caraco), Clozapine (clozaril), Clozapine (fazaclo), Clozapine (ivax), Clozapine (mylan), Clozapine resolution mixture, Clozapine (teva), Clozapine (udl), Clozapine (versacloz), Clozaril, Fazaclo odt, HF 1854, HF-1854, Leponex, NSC-757429, Versacloz, Zaponex)
aldehyde oxidase 1/Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278] There should be some charts here, you may need to enable JavaScript!
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130] α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] 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] α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] There should be some charts here, you may need to enable JavaScript!
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] 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] α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] 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!
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] There should be some charts here, you may need to enable JavaScript!
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608] There should be some charts here, you may need to enable JavaScript!
Calmodulin in Human [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23] Calmodulin in Bovine [ChEMBL: CHEMBL6092] [UniProtKB: P62157] 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] Dopamine D1 receptor in Pig [ChEMBL: CHEMBL5067] [UniProtKB: P50130] Dopamine D1 receptor in Bovine [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] 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!
Dopamine D2 receptor in Chlorocebus aethiops [ChEMBL: CHEMBL5456] [UniProtKB: P52702] D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288] D2 receptor/Dopamine D2 receptor in Mouse [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168] 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!
Dopamine D3 receptor in Chlorocebus aethiops [ChEMBL: CHEMBL2304406] [UniProtKB: P52703] 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!
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] 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!
H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] 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] H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8] There should be some charts here, you may need to enable JavaScript!
H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2] H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1] 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] M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] 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] M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] 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!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] 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 Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] 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] 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] 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] Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] 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] 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] 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] 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] 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] 5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979] 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] 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] 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 in Mouse [GtoPdb: 12] [UniProtKB: P32304] 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!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] There should be some charts here, you may need to enable JavaScript!
Transporter in Rat [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] There should be some charts here, you may need to enable JavaScript!
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] There should be some charts here, you may need to enable JavaScript!
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542] 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
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL	Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis	B	4.36	pIC50	43300	nM	IC50	WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (2018)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor	B	7.43	pKd	37.15	nM	Kd	J Med Chem (1984) 27: 495-503 [PMID:6142954]
ChEMBL	Inhibition of adrenergic alpha1A receptor (unknown origin)	B	7.72	pKi	19	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.72	pKi	19	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	8.3	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL	Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin	B	6.8	pIC50	160	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL	Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.	B	7.66	pKi	22	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.82	pKi	15	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.42	pIC50	38	nM	IC50	DrugMatrix in vitro pharmacology data
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	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	8.2	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL	Displacement of [3H]-prazosin from alpha1B adrenergic receptor in Wistar rat liver membrane after 45 mins by liquid scintillation counting	B	7.54	pKi	29	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]-prozosin from alpha1B adrenoreceptor in rat liver membranes after 45 mins by liquid scintillation counting	B	7.6	pKi	25	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Inhibition of rat adrenergic alpha1B receptor	B	7.92	pKi	12	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	8.44	pKi	3.59	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	8.19	pIC50	6.49	nM	IC50	DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb	-	-	7.7	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	7.77	pKi	17	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	7.46	pIC50	35	nM	IC50	DrugMatrix in vitro pharmacology data
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	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting	B	6.73	pKi	185	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	7.47	pKi	34	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor	B	7.62	pKi	24	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	7.05	pIC50	90	nM	IC50	DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL	Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting	B	7	pKi	100	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.	B	7.72	pKi	19	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	7.96	pKi	11	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	7.64	pIC50	23	nM	IC50	DrugMatrix in vitro pharmacology data
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	Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor	B	8.54	pKi	2.9	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	8.94	pKi	1.14	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	8.1	pIC50	7.88	nM	IC50	DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL	Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.	B	4.59	pKi	26000	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA	B	5	pIC50	>10000	nM	IC50	J Med Chem (1986) 29: 1628-1637 [PMID:2875184]
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
ChEMBL	Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA	B	5	pIC50	>10000	nM	IC50	J Med Chem (1986) 29: 1628-1637 [PMID:2875184]
Calmodulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23]
ChEMBL	Binding affinity to CaM (unknown origin) by equilibrium dialysis method	B	4.7	pIC50	20000	nM	IC50	Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157]
ChEMBL	Binding affinity to bovine brain CaM by FTPFACE analysis	B	4.21	pKd	61000	nM	Kd	Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity towards human Dopamine receptor D1	B	6.27	pKi	540	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human cloned dopamine D1 receptor	B	6.54	pKi	290	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.72	pKi	189	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay	B	6.74	pKi	180	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells	B	6.88	pKi	132	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4543-4547 [PMID:16809034]
ChEMBL	Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells	B	6.88	pKi	132	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4548-4553 [PMID:16806922]
GtoPdb	-	-	6.9	pKi	-	-	-	Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells	B	7.05	pKi	89	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity against dopamine receptor D1	B	7.28	pKi	53	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)	B	7.28	pKi	53	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation	F	7.36	pKi	44	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
ChEMBL	Binding affinity to human dopamine D1 receptor	B	7.36	pKi	44	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	Binding affinity against Dopamine D1 receptor	B	7.5	pKi	31.62	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor	B	7.67	pKi	21.38	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Binding affinity to dopamine D1 receptor (unknown origin)	B	8.12	pKi	7.5	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)	B	6.97	pIC50	107	nM	IC50	DrugMatrix in vitro pharmacology data
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130]
ChEMBL	Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane	B	6.38	pKi	420	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL	Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390	B	6.38	pKi	420	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes	B	6.38	pKi	420	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	Displacement of [3H]SCH23390 from bovine dopamine D1 receptor	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL	Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1	B	6.27	pKi	539	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate	B	6.45	pKi	354.81	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate	B	6.45	pKi	353	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.45	pKi	353	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand	B	6.45	pKi	353	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor	B	6.45	pKi	353	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate	B	6.46	pKi	350	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	pKi value for Dopamine receptor D1 binding site	B	6.5	pKi	316.23	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.	B	6.63	pKi	235	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.68	pKi	210	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.	B	6.77	pKi	170	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.	B	6.77	pKi	169.82	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	In vitro affinity against Dopamine receptor D1	B	6.77	pKi	169.82	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue	B	6.94	pKi	115	nM	Ki	J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL	Binding affinity against dopamine receptor D1	B	6.94	pKi	114.82	nM	Ki	J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL	Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand	B	7.37	pKi	43	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand	B	6.72	pIC50	192	nM	IC50	J Med Chem (1989) 32: 2261-2268 [PMID:2571728]
ChEMBL	Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain	B	6.72	pIC50	192	nM	IC50	J Med Chem (1990) 33: 809-814 [PMID:1967652]
ChEMBL	Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand	B	6.89	pIC50	130	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum	B	6.89	pIC50	130	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.	B	6.89	pIC50	130	nM	IC50	J Med Chem (1995) 38: 4380-4392 [PMID:7473566]
Dopamine D2 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5456] [UniProtKB: P52702]
ChEMBL	Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2	B	6.6	pKi	254	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL	Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D2	B	6.6	pKi	254	nM	Ki	J Med Chem (1995) 38: 2251-2255 [PMID:7783157]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression.	B	6.06	pKi	876	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Displacement of [3H]N-methylspiperone from human cloned D2 dopamine receptor expressed in human fibroblasts incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.37	pKi	431	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Binding affinity to human dopamine D2 receptor	B	6.41	pKi	389	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	Antagonist activity at human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation	F	6.41	pKi	389	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes	B	6.43	pKi	372	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand	B	6.59	pKi	260	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151	B	6.6	pKi	254	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor	B	6.6	pKi	250	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	6.65	pKi	223.87	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	6.65	pKi	223.87	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay	B	6.65	pKi	223.87	nM	Ki	Medchemcomm (2011) 2: 1194-1200
ChEMBL	Displacement of [3H]spiperone from human D2 receptor	B	6.65	pKi	223.87	nM	Ki	Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL	Binding affinity towards dopamine receptor D2	B	6.65	pKi	223.87	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]spiperone human cloned dopamine D2 receptor	B	6.65	pKi	223.87	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells	B	6.66	pKi	220	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Affinity was evaluated as inhibition constant for dopamine D-2 receptor	B	6.66	pKi	220	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin)	B	6.68	pKi	210	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]methylspiperone from dopamine D2 receptor expressed in CHO cells	B	6.68	pKi	208	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4548-4553 [PMID:16806922]
ChEMBL	Displacement of [3H]methylspiperone from human dopamine D2 receptor expressed in CHO cells	B	6.68	pKi	208	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4543-4547 [PMID:16809034]
ChEMBL	Binding affinity towards human D2 dopamine receptor.	B	6.72	pKi	190	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6.72	pKi	190	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement.	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL	Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method	B	6.82	pKi	150	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Binding affinity towards human Dopamine receptor D2	B	6.82	pKi	150	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Inhibition of [3H]-spiperone binding to human Dopamine receptor D2	B	6.84	pKi	144	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity towards human dopamine D2 receptor, using [3H]YM-09151 as a radioligand	B	6.86	pKi	138	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3105-3109 [PMID:12372512]
ChEMBL	Binding affinity towards Dopamine receptor D2 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand	B	6.86	pKi	138	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL	Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test	B	6.87	pKi	134.9	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2	B	6.87	pKi	6.87	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Binding affinity to human cloned dopamine D2 receptor	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Inhibition of D2 receptor (unknown origin)	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	In vitro ability to inhibit the binding of [3H]spiperone to cloned human Dopamine receptor D2 using apomorphine induced climbing test in male Swiss mice	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Binding affinity to human dopamine D2 receptor	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL	DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)	B	6.89	pKi	129	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	6.9	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells	B	6.9	pKi	125.89	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-YM 09151 from D2 receptor	B	6.95	pKi	113	nM	Ki	Bioorg Med Chem Lett (2003) 13: 701-704 [PMID:12639562]
ChEMBL	Binding affinity at human Dopamine receptor D2 by [3H]- YM 09151 displacement.	B	6.95	pKi	113	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2119-2122 [PMID:10999484]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting	B	6.97	pKi	106	nM	Ki	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting	B	6.99	pKi	102.33	nM	Ki	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay	B	7	pKi	>100	nM	Ki	J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL	Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.	B	7.04	pKi	91	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro.	B	7.04	pKi	91	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.05	pKi	89.13	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.05	pKi	88.65	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells	B	7.08	pKi	83	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity against Dopamine receptor D2	B	7.11	pKi	77.62	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines	B	7.13	pKi	74	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells.	B	7.13	pKi	74	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells	B	7.13	pKi	74	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	7.13	pKi	74	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells	B	7.13	pKi	74	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615]
ChEMBL	Competitive antagonist activity against human dopamine D2 receptor short isoform by R-SAT assay	B	7.14	pKi	72	nM	Ki	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
ChEMBL	Binding affinity to human dopamine D2L receptor expressed in HEK293 cells after 1 hr	B	7.14	pKi	72	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	7.15	pKi	71	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity for dopamine receptor D2 determined using [3H]spiperone	B	7.16	pKi	69	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.24	pKi	58.04	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.24	pKi	57.54	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	Binding affinity to human D2R assessed as inhibition constant	B	7.39	pKi	41	nM	Ki	Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL	Binding affinity against dopamine receptor D2L using radioligand [3H]-spiperone	B	7.39	pKi	41	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Displacement of [3H]SCH23390 from human cloned dopamine D2 long receptor expressed in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement.	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D2(long) in CHO cell membrane	B	7.39	pKi	41	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	Ability to displace [3H]SCH-23390 radioligand from cloned human Dopamine receptor D2 in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells	B	7.39	pKi	41	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2L stably expressed in CHO cells	B	7.41	pKi	39	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2L stably expressed in Chinese hamster ovary (CHO) cells was determined.	B	7.41	pKi	39	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	In vitro binding affinity for Dopamine receptor D2	B	7.5	pKi	31.62	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement.	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D2 short receptor expressed in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Binding affinity against dopamine receptor D2S using radioligand [3H]spiperone	B	7.55	pKi	28	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D2 in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2 short form expressed in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D2(short) in CHO cell membrane	B	7.55	pKi	28	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2S expressed in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	Competitive binding affinity against human Dopamine receptor D2S by displacing [3H]spiperone from CHO cells	B	7.55	pKi	28	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2S stably expressed in Chinese hamster ovary (CHO) cells was determined.	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin)	B	8.15	pKi	7.11	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)	B	6.41	pIC50	387	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity towards human Dopamine receptor D2	B	6.59	pIC50	260	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement.	B	6.64	pIC50	230	nM	IC50	J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL	Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay	B	6.69	pIC50	206	nM	IC50	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay	B	6.69	pIC50	204.17	nM	IC50	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Antagonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as inhibition of dopamine-stimulated beta-arrestin2 recruitment measured after 20 to 22 hrs by brightglo-luciferase reporter gene assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2019) 62: 4755-4771 [PMID:30964661]
ChEMBL	Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand	B	6.95	pIC50	113	nM	IC50	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL	Inhibitory concentration against dopamine receptor D2	B	8.05	pIC50	9	nM	IC50	J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL	Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2	B	6.16	pKi	690	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.	B	6.35	pIC50	450	nM	IC50	J Med Chem (1993) 36: 912-918 [PMID:8096548]
ChEMBL	Inhibitory activity against dDopamine receptor D2 in calf caudate tissue, using [3H]spiperone as the radioligand	B	6.6	pIC50	250	nM	IC50	J Med Chem (1989) 32: 2375-2381 [PMID:2571731]
ChEMBL	Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride	B	6.85	pIC50	140	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
ChEMBL	Inhibition of mouse Dopamine receptor D2	B	6.54	pIC50	290	nM	IC50	J Med Chem (1996) 39: 4692-4703 [PMID:8941382]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL	Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand	B	6.1	pKi	790	nM	Ki	J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
GtoPdb	-	-	6.2	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Binding affinity to the dopamine receptor D2L in rat brain membranes	B	6.44	pKi	359	nM	Ki	J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.5	pKi	319	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2	B	6.58	pKi	263.03	nM	Ki	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.	B	6.58	pKi	263.03	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Affinity against Dopamine receptor D2	B	6.58	pKi	263.03	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand	B	6.59	pKi	260	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	pKi value for Dopamine receptor D2 binding site	B	6.6	pKi	251.19	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate	B	6.6	pKi	251.19	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand	B	6.6	pKi	250	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate	B	6.6	pKi	250	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Binding affinity which represents concentration giving half-maximal inhibition of [3H]spiperone (Dopamine receptor D2) binding to rat tissue homogenate	B	6.6	pKi	250	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Inhibition of [3H]spiperone binding to rat dopamine D2 receptor	B	6.6	pKi	250	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.68	pKi	210	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]-N-methylspiperone from rat recombinant dopamine D2 short receptor expressed in CHO cells	B	6.72	pKi	190	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement.	B	6.77	pKi	168	nM	Ki	J Med Chem (1993) 36: 3073-3076 [PMID:7901415]
ChEMBL	Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Binding affinity at dopamine D2 receptor in rat striatal membranes	B	6.84	pKi	144.54	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534]
ChEMBL	Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting	B	6.85	pKi	140	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Binding affinity of [3H]spiperone towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain	B	6.86	pKi	138	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting	B	6.88	pKi	130.7	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum	B	6.88	pKi	130.7	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum tissue after 20 mins by scintillation counting	B	6.89	pKi	130	nM	Ki	Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL	Displacement of [3H]-YM-09151-2 from D2 dopamine receptor in Wistar rat brain striatal membrane after 60 mins by liquid scintillation counting	B	6.89	pKi	130	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis	B	6.89	pKi	128.7	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	In vitro Dopamine receptor D2 affinity by using [3H]spiperone as the radioligand in rat limbic system at 1 uM concentration of compound; value may range from 113 to 362	B	6.93	pKi	118	nM	Ki	J Med Chem (1987) 30: 1818-1823 [PMID:2888898]
ChEMBL	Displacement of [3H]spiperone from Dopamine receptor D2 of rat corpora striata synaptic membranes	B	6.93	pKi	117	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL	Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane	B	7	pKi	100	nM	Ki	Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL	Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding.	B	7.03	pKi	93	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H]NPA from rat brain Dopamine receptor D2	B	7.08	pKi	83.18	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Displacement of [3H]NPA from rat brain Dopamine receptor D2	B	7.08	pKi	83	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain	B	7.09	pKi	82	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations	B	7.09	pKi	82	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Binding affinity against Dopamine receptor D2 from rat striatum	B	7.09	pKi	82	nM	Ki	J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	7.19	pKi	64.2	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	7.2	pKi	63.1	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Binding affinity of [3H]U-86170 towards Dopamine receptor D2 in cloned mammalian receptor expressed in cultured cells or from rat whole brain	B	7.26	pKi	55	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum	B	7.27	pKi	53.6	nM	Ki	J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL	Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone	B	7.27	pKi	53.6	nM	Ki	J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL	Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone	B	7.27	pKi	53.6	nM	Ki	J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL	Binding affinity against dopamine D2 receptor	B	7.34	pKi	45.71	nM	Ki	J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL	In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue.	B	7.35	pKi	45	nM	Ki	J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL	In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound	B	7.47	pKi	34	nM	Ki	J Med Chem (1987) 30: 1818-1823 [PMID:2888898]
ChEMBL	In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone	B	7.47	pKi	34	nM	Ki	J Med Chem (1987) 30: 1100-1105 [PMID:2884314]
ChEMBL	Binding activity against dopamine D2 receptor in rat brain, using [3H]spiperone as the radioligand	B	5.56	pIC50	2770	nM	IC50	J Med Chem (1989) 32: 2261-2268 [PMID:2571728]
ChEMBL	Binding affinity for Dopamine receptor D2 using [3H]spiperone in rat brain	B	5.56	pIC50	2770	nM	IC50	J Med Chem (1990) 33: 809-814 [PMID:1967652]
ChEMBL	In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand	B	5.68	pIC50	2108	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL	In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum	B	5.79	pIC50	1610	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand	B	5.79	pIC50	1610	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue	B	6	pIC50	1000	nM	IC50	J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL	Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum.	B	6.08	pIC50	830	nM	IC50	J Med Chem (1995) 38: 1119-1131 [PMID:7707315]
ChEMBL	In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2	B	6.36	pIC50	440	nM	IC50	J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL	Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone	B	6.36	pIC50	440	nM	IC50	J Med Chem (1986) 29: 359-369 [PMID:2869146]
ChEMBL	Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone	B	6.36	pIC50	440	nM	IC50	J Med Chem (1989) 32: 1147-1156 [PMID:2542551]
ChEMBL	Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2	B	6.39	pIC50	410	nM	IC50	J Med Chem (1992) 35: 1092-1101 [PMID:1348090]
ChEMBL	Ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat corpus striatum	B	6.4	pIC50	400	nM	IC50	J Med Chem (1988) 31: 618-624 [PMID:2894466]
ChEMBL	Binding affinity against dopamine receptor D2	B	6.48	pIC50	330	nM	IC50	J Med Chem (1995) 38: 4380-4392 [PMID:7473566]
ChEMBL	Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand	B	6.48	pIC50	330	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum	B	6.48	pIC50	330	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats	B	6.54	pIC50	290	nM	IC50	J Med Chem (1994) 37: 2552-2563 [PMID:7914539]
ChEMBL	Inhibition of [3H]raclopride binding at Dopamine receptor D2 from rat striata.	B	6.54	pIC50	290	nM	IC50	J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL	Inhibition of [3H]spiperone binding to Dopamine receptor D2 from striatum of the rat brain	B	6.6	pIC50	250	nM	IC50	J Med Chem (1989) 32: 2573-2582 [PMID:2573732]
ChEMBL	Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand.	B	6.76	pIC50	172	nM	IC50	J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL	Inhibition of spiropiperidone binding at dopamine receptor D2 of rat.	B	6.88	pIC50	132	nM	IC50	J Med Chem (2001) 44: 372-389 [PMID:11462978]
ChEMBL	Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2	B	6.89	pIC50	130	nM	IC50	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	In vitro binding affinity against Dopamine receptor D2 by displacement of [3H]haloperidol from rat striatal membranes.	B	7.42	pIC50	38	nM	IC50	J Med Chem (1987) 30: 1807-1812 [PMID:2888897]
Dopamine D3 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304406] [UniProtKB: P52703]
ChEMBL	Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3	B	6.33	pKi	466	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Competitive binding affinity against human Dopamine receptor D3 by displacing [3H]spiperone from CHO cells	B	6.02	pKi	960	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone	B	6.02	pKi	960	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D3 in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Binding affinity evaluated for the displacement of [3H]-spiperone against human dopamine receptor D3	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D3 stably expressed in CHO cells by [3H]spiperone displacement.	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Ability to displace [3H]spiperone from the cloned human D3 dopamine receptor stably expressed in Chinese hamster ovary (CHO) cells was determined.	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D3 in CHO cell membrane	B	6.02	pKi	960	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor expressed in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Displacement of [3H]-spiperone from human D3 receptor assessed as inhibition constant	B	6.02	pKi	960	nM	Ki	Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor	B	6.04	pKi	912.01	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Displacement of [3H]N-methylspiperone from human cloned D3 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.19	pKi	646	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding.	B	6.29	pKi	513	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
GtoPdb	-	-	6.3	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]
ChEMBL	Binding affinity on human Dopamine receptor D3 expressed in CHO cells using radioligand [3H]-YM 09151	B	6.34	pKi	454	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Binding affinity to dopamine D3 receptor	B	6.43	pKi	372.3	nM	Ki	J Nat Prod (2010) 73: 1015-1021 [PMID:20408551]
ChEMBL	Binding affinity towards human Dopamine receptor D3	B	6.44	pKi	360	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin)	B	6.5	pKi	319	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells	B	6.5	pKi	319	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry	B	6.5	pKi	319	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	B	6.53	pKi	295	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity towards human dopamine receptor D3	B	6.55	pKi	280	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3	B	6.62	pKi	242	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity to human cloned dopamine D3 receptor	B	6.62	pKi	240	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	In vitro ability to inhibit the binding of [3H]7-OH-DPAT to cloned human Dopamine receptor D3 using apomorphine induced climbing test in male Swiss mice	B	6.62	pKi	240	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]7-OH-DPAT from human Dopamine receptor D3	B	6.62	pKi	6.62	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test	B	6.62	pKi	239.88	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro.	B	6.65	pKi	222	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.	B	6.65	pKi	222	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in HEK293 cells	B	6.7	pKi	200	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells	B	6.7	pKi	200	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	6.7	pKi	200	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D3 stably expressed in HEK393 cell lines	B	6.7	pKi	200	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	6.7	pKi	200	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells	B	7.06	pKi	88	nM	Ki	J Med Chem (2003) 46: 4377-4392 [PMID:14521403]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	7.06	pKi	88	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity towards human Dopamine receptor D3	B	6.35	pIC50	450	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	6.59	pIC50	258	nM	IC50	DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb	-	-	5.7	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Binding affinity towards baculovirus expressed rat dopamine D3 receptors	B	6.3	pKi	500	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle	B	6.47	pKi	340.1	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate	B	6.49	pKi	320	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand	B	6.5	pKi	319	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand	B	6.55	pKi	280	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting	B	6.58	pKi	260.1	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis	B	6.62	pKi	239.8	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand	B	6.64	pKi	230	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	6.73	pKi	188	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	6.79	pKi	161	nM	Ki	Med Chem Res (2004) 13: 25-33
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand	B	5.05	pKi	9000	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL	Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor	B	7.14	pKi	72	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL	Displacement of [3H]-YM 09151 from human Dopamine receptor D4	B	7.15	pKi	71	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL	Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151	B	7.15	pKi	70	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting	B	7.22	pKi	60	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting	B	7.22	pKi	60	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice	B	7.27	pKi	54	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Binding affinity to human cloned dopamine D4 receptor	B	7.27	pKi	54	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4	B	7.27	pKi	7.27	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test	B	7.27	pKi	53.7	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.	B	7.33	pKi	47	nM	Ki	Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL	Displacement of radiolabeled clozapine from human dopamine D4.4 receptor	B	7.36	pKi	44	nM	Ki	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Binding affinity towards human dopamine-4.2 receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity towards human dopamine receptor D4	B	7.4	pKi	40	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Inhibition of human dopamine D4 receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells	B	7.4	pKi	39.81	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand	B	7.41	pKi	39	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay	B	7.41	pKi	39	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.	B	7.44	pKi	36	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
GtoPdb	-	-	7.5	pKi	-	-	-	Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973]
ChEMBL	In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4	B	7.52	pKi	30.4	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL	In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.	B	7.52	pKi	30	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand	B	7.52	pKi	30	nM	Ki	J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL	Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells	B	7.52	pKi	30	nM	Ki	J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL	In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4	B	7.55	pKi	28.4	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL	Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells	B	7.68	pKi	21	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Affinity was evaluated as inhibition constant for dopamine D-4 receptor	B	7.68	pKi	21	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting	B	7.74	pKi	18	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes	B	7.74	pKi	18	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	Displacement of [3H]-YM 09151 from D4 receptor	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem Lett (2003) 13: 701-704 [PMID:12639562]
ChEMBL	Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2119-2122 [PMID:10999484]
ChEMBL	Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells	B	7.77	pKi	17	nM	Ki	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells	B	7.77	pKi	17	nM	Ki	Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL	Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro	B	7.8	pKi	16	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane	B	7.8	pKi	16	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells	B	7.8	pKi	16	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone	B	7.8	pKi	16	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone	B	7.8	pKi	16	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins	B	7.8	pKi	16	nM	Ki	Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL	Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	In vitro binding affinity for Dopamine receptor D4	B	7.8	pKi	15.85	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
ChEMBL	Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells	B	7.8	pKi	7.8	D4	Log Ki	J Med Chem (2001) 44: 1151-1157 [PMID:11312915]
ChEMBL	Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay	B	7.82	pKi	15	nM	Ki	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells	B	7.89	pKi	13	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL	Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Inhibition of human dopamine D4 receptor	B	8	pKi	10	nM	Ki	J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.	B	8	pKi	10	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Binding affinity towards human Dopamine receptor D4.2 in CHO cells	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines	B	8	pKi	10	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells	B	8	pKi	10	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615]
ChEMBL	Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand	B	8.05	pKi	9	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3105-3109 [PMID:12372512]
ChEMBL	Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation	F	6.77	pIC50	168	nM	IC50	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	Percent inhibition against Dopamine receptor D4 at 1 uM	B	6.81	pIC50	156	nM	IC50	J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL	Inhibitory concentration against dopamine receptor D4	B	6.86	pIC50	138	nM	IC50	J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL	Inhibition of human dopamine D4.4 receptor	B	6.92	pIC50	120	nM	IC50	Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL	Displacement of radiolabeled clozapine from human dopamine D4.4 receptor	B	6.96	pIC50	110	nM	IC50	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells	B	7.24	pIC50	58	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Binding affinity towards human D4.2 receptor	B	7.28	pIC50	52	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells	B	7.39	pIC50	41	nM	IC50	Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL	Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay	B	7.4	pIC50	40	nM	IC50	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay	B	7.49	pIC50	32	nM	IC50	Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.	B	7.64	pIC50	23	nM	IC50	J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL	Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand	B	7.77	pIC50	17	nM	IC50	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL	Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.	B	7.49	pKi	32	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain	B	7.54	pKi	29	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain	B	8.05	pKi	9	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL	Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay	B	6.11	pKi	780	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
GtoPdb	-	-	6.6	pKi	-	-	-	Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL	Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.63	pKi	235	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells	B	6.7	pKi	198	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL	Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor	B	6	pIC50	>1000	nM	IC50	J Med Chem (1986) 29: 359-369 [PMID:2869146]
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	4.77	pKi	17000	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Binding affinity to human ERG expressed in HEK293 cells	B	4.77	pKi	17000	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)	B	5.06	pKi	8660.6	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay	B	5.39	pKi	4060	nM	Ki	J Med Chem (2007) 50: 2931-2941 [PMID:17536794]
ChEMBL	Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA	B	5.51	pKi	3080	nM	Ki	J Med Chem (2007) 50: 2931-2941 [PMID:17536794]
ChEMBL	DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)	B	4.98	pIC50	10571	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel)	F	5.24	pIC50	5754.4	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL	Inhibition of human ERG	B	5.4	pIC50	3981.07	nM	IC50	Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL	Inhibition of human ERG	B	5.49	pIC50	3200	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	Inhibition of human ERG	B	6.05	pIC50	901	nM	IC50	Medchemcomm (2015) 6: 831-838
ChEMBL	Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay	B	6.19	pIC50	650	nM	IC50	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL	Inhibition of human Potassium channel HERG expressed in mammalian cells	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL	Inhibitory concentration against potassium channel HERG	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL	Inhibition of human ERG channel	B	6.49	pIC50	320	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	Inhibition of human ERG channel	B	6.49	pIC50	320	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1	F	6.72	pIC50	191	nM	IC50	J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL	Inhibition of human ERG in MCF7 cells	B	6.72	pIC50	190.55	nM	IC50	Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL	Binding affinity to human histamine H1 receptor	B	8.51	pKd	3.1	nM	Kd	J Med Chem (2011) 54: 26-53 [PMID:21062081]
ChEMBL	Binding affinity against histamine H1 receptor	B	7.77	pKi	17	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells	B	8.62	pKi	2.38	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity towards human histamine H1 receptor	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human cloned histamine H1 receptor	B	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting	B	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	9	pKi	1	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Inhibition of histamine H1 receptor (unknown origin)	B	9	pKi	1	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	9.24	pKi	0.57	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	9.6	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734]
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	8.31	pIC50	4.91	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inverse agonist activity at human histamine H1 receptor by R-SAT assay	B	9.4	pEC50	0.4	nM	EC50	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL	Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate	B	7.85	pKi	14	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.	B	8.3	pKi	5	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine	B	8.54	pKi	2.9	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand	B	7.64	pIC50	23	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes	B	7.64	pIC50	23	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Displacement of [3H]mepyramine from H1R in rat brain	B	8.05	pIC50	9	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]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting	B	7.91	pKi	12.2	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum	B	8.09	pKi	8.1	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting	B	8.17	pKi	6.8	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis	B	8.42	pKi	3.8	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	B	5.45	pKi	3550	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	B	5.44	pIC50	3610	nM	IC50	DrugMatrix in vitro pharmacology data
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL	Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Antagonist potency against human H3 receptor in GTPgamma-S-Assay	F	6.2	pKi	631	nM	Ki	J Med Chem (2005) 48: 306-311 [PMID:15634025]
H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8]
GtoPdb	-	-	5.8	pKi	-	-	-	J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM	B	7.15	pKd	70.2	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM	B	7.68	pKd	20.9	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM	B	7.84	pKd	14.5	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells	B	7.92	pKd	11.9	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis	B	6.3	pKi	501.19	nM	Ki	Medchemcomm (2013) 4: 193-204
ChEMBL	Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting	B	6.7	pKi	199.53	nM	Ki	J Med Chem (2011) 54: 8136-8147 [PMID:22003888]
GtoPdb	-	-	6.7	pKi	-	-	-	Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436]; J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells	B	6.75	pKi	177.83	nM	Ki	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2]
GtoPdb	-	-	5.5	pKi	-	-	-	J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]
H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1]
GtoPdb	-	-	5.7	pKi	-	-	-	J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells	B	8.2	pKi	6.31	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8.61	pKi	2.47	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to human cloned muscarinic M1 receptor	B	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting	B	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Binding affinity towards human M1 muscarinic receptor.	B	9.01	pKi	0.98	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
GtoPdb	-	-	7.9	pIC50	-	-	-	Proc Natl Acad Sci USA (2003) 100: 13674-9 [PMID:14595031]
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8	pIC50	10	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells	B	8.03	pIC50	9.4	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells	B	8.03	pIC50	9.4	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL	Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate	B	7.26	pKi	55	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB	B	7.27	pKi	54	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by radioligand [3H]pirenzepine binding assay.	B	8.68	pKi	2.1	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
GtoPdb	-	-	7.7	pIC50	-	-	-	Mol Pharmacol (2006) 70: 1974-83 [PMID:16959945]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL	DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	6.77	pKi	169	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to M2 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	6.32	pIC50	476	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at muscarinic M2 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL	Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by Radio ligand [3H]quinuclidinyl binding assay.	B	7.34	pKi	46	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.77	pKi	17	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.11	pIC50	78	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells	B	7.9	pKi	12.59	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8.2	pKi	6.3	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.35	pIC50	45	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at muscarinic M4 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8.02	pKi	9.53	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.89	pIC50	13	nM	IC50	DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.84	pKi	1458	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.83	pIC50	1470	nM	IC50	DrugMatrix in vitro pharmacology data
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter	B	6.16	pKi	697	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay	F	4.9	pIC50	12589.25	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay	F	5	pIC50	10000	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay	F	5.1	pIC50	7943.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay	F	5.1	pIC50	7943.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	5.4	pIC50	3981.07	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 1 receptor	B	6.15	pKi	710	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity against 5-Hydroxytryptamine 1A receptor	B	6.38	pKi	416.87	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand	B	6.57	pKi	270	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
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	6.74	pKi	180	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Binding affinity to 5HT1A receptor (unknown origin)	B	6.8	pKi	160	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 HEK293 cells after 1 hr	B	6.84	pKi	143	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	6.84	pKi	143	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr	B	6.84	pKi	143	nM	Ki	Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101]
ChEMBL	Binding affinity to human cloned 5HT1A receptor	B	6.85	pKi	140	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Inhibition of human 5HT1A receptor	B	6.85	pKi	140	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
GtoPdb	-	-	6.9	pKi	-	-	-	Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]
ChEMBL	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells after 60 mins by liquid scintillation counting	B	7	pKi	101	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity to human 5HT1A receptor	B	8.05	pKi	8.9	nM	Ki	Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL	Binding affinity to 5-HT1A receptor (unknown origin)	B	8.2	pKi	6.38	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT	B	6.82	pIC50	150	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL	Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice.	B	5.7	pIC50	2000	nM	IC50	J Med Chem (1996) 39: 4692-4703 [PMID:8941382]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand	B	6.19	pKi	640	nM	Ki	J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine receptor 1A receptor by using [3H]8-OH-DPAT in rat hippocampal membranes.	B	6.35	pKi	443	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M.	B	6.38	pKi	415	nM	Ki	J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL	Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate	B	6.42	pKi	380	nM	Ki	Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	6.55	pKi	281	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]-OH-8-DPAT from 5HT1A receptor in Wistar rat hippocampal membrane after 15 mins by liquid scintillation counting	B	6.59	pKi	260	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat brain hippocampal membranes after 15 mins by liquid scintillation counting	B	6.59	pKi	260	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding.	B	6.61	pKi	247	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat brain cortex	B	6.73	pKi	185.6	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting	B	6.73	pKi	185.6	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting	B	6.79	pKi	161	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry	B	6.8	pKi	160	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	6.8	pKi	160	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Binding affinity of [3H]-8-OH-DPAT towards 5-hydroxytryptamine 1A receptor in cloned mammalian receptor expressed in cultured cells or from rat whole brain.	B	6.82	pKi	150	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis	B	6.85	pKi	141.6	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A in rat brain cerebral cortex after 15 mins by scintillation counting	B	6.85	pKi	140	nM	Ki	Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL	Compound was tested for the Binding affinity against rat hippocampal 5-hydroxytryptamine 1A receptor by Radio ligand [3H]8-OH-DPAT binding assay.	B	6.89	pKi	130	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations	B	6.95	pKi	111	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Compound was evaluated for its binding affinity against 5-hydroxytryptamine 1A receptor from rat cerebral cortex	B	6.95	pKi	111	nM	Ki	J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL	Binding affinity at 5HT1A receptor in rat striatal membranes	B	7.02	pKi	95.5	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534]
ChEMBL	Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101	B	7.41	pKi	39	nM	Ki	J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL	The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus	B	7.41	pKi	39	nM	Ki	J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL	Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101.	B	7.41	pKi	38.5	nM	Ki	J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL	In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin	B	5.7	pIC50	2000	nM	IC50	J Med Chem (1994) 37: 2552-2563 [PMID:7914539]
ChEMBL	Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue.	B	5.7	pIC50	2000	nM	IC50	J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL	In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus	B	5.99	pIC50	1015.5	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand	B	6	pIC50	1010	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand.	B	6.22	pIC50	600	nM	IC50	J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL	Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue	B	6.24	pIC50	580	nM	IC50	J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	6.31	pIC50	491	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand	B	6.57	pIC50	267.6	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
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	-	-	6.2	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	6.02	pKi	959	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT	B	5.6	pIC50	2500	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	5.68	pIC50	2109	nM	IC50	DrugMatrix in vitro pharmacology data
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	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.4	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
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
GtoPdb	-	-	6.4	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Binding affinity to human 5HT2A receptor	B	6.64	pKi	230	nM	Ki	Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	7.44	pKi	36.31	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	7.44	pKi	36	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
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	7.48	pKi	33	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method	B	7.62	pKi	24	nM	Ki	J Nat Prod (2022) 85: 2149-2158 [PMID:36001775]
ChEMBL	Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membranes by radioligand binding assay	B	7.74	pKi	18	nM	Ki	J Nat Prod (2015) 78: 722-729 [PMID:25695425]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method	B	7.79	pKi	16.1	nM	Ki	Medchemcomm (2018) 9: 1069-1075 [PMID:30108996]
ChEMBL	Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method	B	7.82	pKi	15	nM	Ki	Medchemcomm (2015) 6: 601-605
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor measured after 90 mins by microbeta scintillation counting method	B	7.82	pKi	15	nM	Ki	Bioorg Med Chem Lett (2016) 26: 3216-3219 [PMID:27261181]
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method	B	7.89	pKi	13	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity to 5HT2A receptor (unknown origin)	B	8	pKi	10	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
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	Displacement of [125]DOI from human recombinant full length 5HT2A receptor expressed in HEK293E cells	B	8.02	pKi	9.6	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	8.02	pKi	9.6	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	8.04	pKi	9.12	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor	B	8.04	pKi	9.12	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	8.04	pKi	9.12	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor	B	8.04	pKi	9.12	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay	B	8.04	pKi	9.12	nM	Ki	Medchemcomm (2011) 2: 1194-1200
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor	B	8.04	pKi	9.12	nM	Ki	Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	8.04	pKi	9.12	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	8.04	pKi	9.1	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Binding affinity to human cloned 5HT2A receptor	B	8.05	pKi	8.9	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding affinity to 5-HT2A receptor (unknown origin)	B	8.07	pKi	8.57	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand	B	8.11	pKi	7.8	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)	B	8.13	pKi	7.41	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)	B	8.14	pKi	7.3	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity to 5-HT2A receptor (unknown origin)	B	8.27	pKi	5.35	nM	Ki	Bioorg Med Chem Lett (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL	Antagonist activity at 5HT2A receptor (unknown origin)	B	8.27	pKi	5.35	nM	Ki	Eur J Med Chem (2020) 193: 112214-112214 [PMID:32182489]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity towards human 5-HT2A receptor in BEK cells	B	8.3	pKi	5	nM	Ki	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting	B	8.32	pKi	4.84	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	Binding affinity for human 5-hydroxytryptamine 2A receptor	B	8.4	pKi	4	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human 5HT2A receptor	B	8.52	pKi	3.03	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165]
ChEMBL	Displacement of [3H]-Ketanserin from 5-HT2A receptor (unknown origin) incubated for 90 mins by microbeta counting method	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Binding affinity against 5-Hydroxytryptamine 2A receptor	B	8.57	pKi	2.69	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity to human 5HT2A receptor	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	8.92	pKi	1.2	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	9	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]
ChEMBL	Inhibitory concentration against human 5-HT2A receptor in BEK cells	B	7.92	pIC50	12	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	8.38	pIC50	4.2	nM	IC50	DrugMatrix in vitro pharmacology data
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
ChEMBL	Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin	B	8.52	pIC50	3	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL	Compound was tested for Antagonistic activity against denuded rat aorta	F	8.62	pKd	2.4	nM	Kd	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	Negative log concentration of antagonist on 5-hydroxytryptamine 2A receptor in rat thoracic aorta	F	9.16	pKd	0.69	nM	Kd	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor	B	7.56	pKi	27.54	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by liquid scintillation counting	B	7.68	pKi	21	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting	B	7.7	pKi	20	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay.	B	7.77	pKi	17	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor	B	7.82	pKi	15.14	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting	B	7.84	pKi	14.5	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652]
ChEMBL	Binding affinity at 5HT2A receptor in rat striatal membranes	B	7.88	pKi	13.18	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534]
ChEMBL	Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting	B	7.89	pKi	12.9	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat brain cortex	B	7.89	pKi	12.9	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis	B	7.94	pKi	11.6	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand	B	8	pKi	10	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry	B	8	pKi	10	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate	B	8	pKi	10	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry	B	8	pKi	10	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate	B	8	pKi	10	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor	B	8	pKi	10	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding.	B	8.03	pKi	9.4	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2A receptor	B	8.05	pKi	9	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A in rat brain cerebral cortex after 20 mins by scintillation counting	B	8.05	pKi	8.9	nM	Ki	Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL	Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor.	B	8.1	pKi	8	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2A receptor	B	8.1	pKi	8	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor)	B	8.12	pKi	7.59	nM	Ki	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex	B	8.12	pKi	7.59	nM	Ki	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane	B	8.17	pKi	6.7	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membrane	B	8.22	pKi	6.05	nM	Ki	Eur J Med Chem (2009) 44: 800-808 [PMID:18603331]
ChEMBL	Tested in vitro for its ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat frontal cortex membranes	B	8.3	pKi	5.01	nM	Ki	Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL	In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.	B	8.3	pKi	5.01	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Affinity at 5-hydroxytryptamine 2A receptor of the rat brain cortex was assessed on the basis of their ability to displace [3H]ketanserin	B	8.8	pKi	1.58	nM	Ki	J Med Chem (2000) 43: 1901-1909 [PMID:10821703]
GtoPdb	-	-	8.9	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL	In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex	B	7.14	pIC50	72	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand	B	7.39	pIC50	40.7	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL	Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor	B	7.89	pIC50	13	nM	IC50	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand	B	7.92	pIC50	12	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain	B	8.11	pIC50	7.8	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.	B	8.11	pIC50	7.8	nM	IC50	J Med Chem (1995) 38: 4380-4392 [PMID:7473566]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	Displacement of [3H]-5HT from human 5-HT2B receptor expressed in african green monkey COS7 cells assessed as inhibition constant	B	8.14	pKi	7.2	nM	Ki	J Med Chem (2023) 66: 11027-11039 [PMID:37584406]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	8.14	pKi	7.18	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells	B	8.5	pKi	3.16	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb	-	-	8.8	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	7.96	pIC50	11	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inverse agonist activity at human 5HT2B receptor by R-SAT assay	B	7.7	pEC50	20	nM	EC50	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL	Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus	F	6.77	pKd	169.82	nM	Kd	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor	F	6.9	pKd	125.89	nM	Kd	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	7.14	pKi	73	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	7.14	pKi	72.44	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting	B	7.62	pKi	24	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting	B	7.64	pKi	23	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor	B	7.68	pKi	21	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity to human cloned 5HT2C receptor	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.	B	7.8	pKi	15.85	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus	B	7.8	pKi	15.85	nM	Ki	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells	B	7.82	pKi	15	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.89	pKi	13	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [125]DOI from human recombinant full length 5HT2C receptor expressed in HEK293E cells	B	7.89	pKi	13	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor	B	7.89	pKi	13	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Displacement of [3H]mesulergine from human cloned 5HT2C receptor	B	7.98	pKi	10.47	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	8.03	pKi	9.33	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	8.03	pKi	9.3	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 2C receptor	B	8.3	pKi	5	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity to 5HT2C receptor (unknown origin)	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	8.5	pKi	3.16	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity against 5-Hydroxytryptamine 2C receptor	B	8.54	pKi	2.88	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity to 5-HT2C receptor (unknown origin)	B	8.54	pKi	2.88	nM	Ki	Med Chem Res (2013) 22: 520-530
GtoPdb	-	-	8.7	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]; J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]; J Neurochem (1999) 72: 2127-34 [PMID:10217294]
ChEMBL	Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine	B	8	pIC50	10	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	8.22	pIC50	6.04	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inverse agonist activity at human 5HT2C receptor by R-SAT assay	B	6.6	pEC50	250	nM	EC50	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
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 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting	B	7.38	pKi	41.9	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor in rat brain cortex	B	7.48	pKi	33.1	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Compound was evaluated for its binding affinity towards rat r5-hydroxytryptamine 2C receptor	B	7.64	pKi	23	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis	B	7.79	pKi	16.2	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2C receptor	B	8.1	pKi	8	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2C serotonin receptor.	B	8.1	pKi	8	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand	B	7.96	pIC50	11	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes	B	7.96	pIC50	11	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
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	6.4	pKi	398.11	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL	Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 3 receptor	B	7.28	pKi	53	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
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
ChEMBL	Binding affinity against 5-Hydroxytryptamine 3 receptor	B	6.73	pKi	186.21	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity to 5-HT3 receptor (unknown origin)	B	6.73	pKi	186.21	nM	Ki	Med Chem Res (2013) 22: 520-530
5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
ChEMBL	Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay.	B	7.49	pKi	32	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand	B	6	pKi	1000	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.5	pKi	-	-	-	FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb	-	-	5.3	pKi	-	-	-	Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
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	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity for human 5-hydroxytryptamine 6 receptor	B	7.3	pKi	<50	nM	Ki	J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	B	7.77	pKi	17	nM	Ki	J Med Chem (2012) 55: 5704-5719 [PMID:22537153]
ChEMBL	Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL	Binding affinity to human cloned 5HT6 receptor	B	7.96	pKi	11	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation	F	8	pKi	<10	nM	Ki	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor	B	8	pKi	10	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand	B	8.02	pKi	9.5	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb	-	-	8.1	pKi	-	-	-	J Neurochem (1996) 66: 47-56 [PMID:8522988]; Mol Pharmacol (1998) 54: 577-83 [PMID:9730917]; Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]; Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)	B	8.21	pKi	6.1	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)	B	8.22	pKi	6.03	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	8.3	pKi	5.05	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand	B	8.32	pKi	4.8	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2295-2299 [PMID:11055342]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr	B	8.4	pKi	4	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101]
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	8.4	pKi	4	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 6 receptor	B	8.4	pKi	4	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay	F	7.69	pIC50	20.3	nM	IC50	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay	F	7.7	pIC50	20	nM	IC50	J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL	Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells	B	7.77	pIC50	17	nM	IC50	Bioorg Med Chem (2014) 22: 1782-1790 [PMID:24495863]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	7.96	pIC50	11	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb	-	-	8.4	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]; Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]; Neuropharmacology (1997) 36: 713-20 [PMID:9225298]; J Neurochem (1998) 71: 2169-77 [PMID:9798944]; Mol Pharmacol (1998) 54: 577-83 [PMID:9730917]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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	5	pKi	>10000	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
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]-5-CT from 5-HT7 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay	B	7.21	pKi	62	nM	Ki	J Med Chem (2024) 67: 1580-1610 [PMID:38190615]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method	B	7.32	pKi	48.4	nM	Ki	Eur J Med Chem (2019) 179: 1-15 [PMID:31229883]
ChEMBL	Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor	B	7.32	pKi	48	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method	B	7.32	pKi	47.86	nM	Ki	Eur J Med Chem (2019) 179: 1-15 [PMID:31229883]
ChEMBL	Displacement of [3H]-5-CT from human recombinant 5-HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method	B	7.32	pKi	47.4	nM	Ki	Eur J Med Chem (2019) 170: 261-275 [PMID:30904783]
ChEMBL	Displacement of [3H]-5-CT from 5-HT7b receptor (unknown origin)	B	7.34	pKi	45.5	nM	Ki	ACS Med Chem Lett (2017) 8: 390-394 [PMID:28435524]
ChEMBL	Displacement of [3H]-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis	B	7.34	pKi	45.5	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
ChEMBL	Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Displacement of [3H]5CT from 5HT7 receptor	B	7.4	pKi	39.81	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2465-2468 [PMID:20346662]
ChEMBL	Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cell membranes by radioligand binding assay	B	7.43	pKi	37	nM	Ki	J Nat Prod (2015) 78: 722-729 [PMID:25695425]
ChEMBL	Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis	B	7.6	pKi	25	nM	Ki	Eur J Med Chem (2014) 78: 324-339 [PMID:24691057]
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	7.68	pKi	21	nM	Ki	Eur J Med Chem (2022) 232: 114193-114193 [PMID:35176563]
ChEMBL	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	B	7.7	pKi	19.95	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	7.74	pKi	18	nM	Ki	Medchemcomm (2018) 9: 1033-1044 [PMID:30108992]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2019) 178: 740-751 [PMID:31229876]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2019) 180: 383-397 [PMID:31325785]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2020) 201: 112437-112437 [PMID:32673902]
ChEMBL	Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101]
ChEMBL	Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem (2015) 23: 212-221 [PMID:25435254]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2016) 112: 258-269 [PMID:26900658]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2018) 147: 102-114 [PMID:29425815]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
GtoPdb	-	-	7.8	pKi	-	-	-	Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958]; Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657]; Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804]
ChEMBL	Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor	B	7.9	pKi	12.59	nM	Ki	J Med Chem (2003) 46: 5638-5650 [PMID:14667218]
ChEMBL	Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method	B	7.94	pKi	11.4	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 7 receptor	B	8.05	pKi	9	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)	B	8.23	pKi	5.89	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)	B	8.26	pKi	5.5	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb	-	-	7.4	pKi	-	-	-	Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]
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 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting	B	7.2	pKi	62.6	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 7 receptor	B	7.9	pKi	12.59	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226]
GtoPdb	-	-	8.2	pKi	-	-	-	Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
ChEMBL	Binding affinity towards rat 5-hydroxytryptamine 7 receptor	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Binding affinity to human SERT	B	5.41	pKi	3900	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6	pKi	>1000	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	6.54	pKi	290	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of 5-HT uptake at SERT (unknown origin)	B	5	pIC50	>10000	nM	IC50	Med Chem Res (2013) 22: 520-530
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	6.26	pIC50	546	nM	IC50	DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Inhibitory concentration against reuptake of 5-HT from rat synaptosomes	F	5	pIC50	>10000	nM	IC50	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain	B	5.07	pKi	8500	nM	Ki	J Med Chem (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL	Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding.	B	5.07	pKi	8500	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL	Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor	B	6	pIC50	>1000	nM	IC50	J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Binding affinity to rat NET	B	6.41	pKi	390	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb	-	-	6.9	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb	-	-	3.8	pEC50	-	-	-	Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978]

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]