pimozide [Ligand Id: 90] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1423 (MCN-JR-6238, NSC-170984, Orap, Pimozide, R 623, R-623, R 6238, R-6238)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor in Rat [GtoPdb: 215] [UniProtKB: P61169]
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  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
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  • 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]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • Nav1.2/Sodium channel protein type II alpha subunit in Rat [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1 in Human [ChEMBL: CHEMBL1795087] [GtoPdb: 2428] [UniProtKB: O94782]
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  • ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3]
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  • Cav3.1/Voltage-gated T-type calcium channel alpha-1G subunit in Human [ChEMBL: CHEMBL4641] [GtoPdb: 535] [UniProtKB: O43497]
  • Cav3.1 in Rat [GtoPdb: 535] [UniProtKB: O54898]
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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  • Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
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  • Cav3.2 in Human [GtoPdb: 536] [UniProtKB: O95180]
  • Cav3.2 in Rat [GtoPdb: 536] [UniProtKB: Q9EQ60]
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  • Cav3.3 in Human [GtoPdb: 537] [UniProtKB: Q9P0X4]
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  • Kv1.8 in Human [GtoPdb: 545] [UniProtKB: Q16322]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Binding affinity against delta opiate receptor using [3H]DPDPE B 5.42 pIC50 3760 nM IC50 J Med Chem (2001) 44: 3391-3401 [PMID:11585444]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Inhibition of dopamine D2 receptor B 7.54 pKd 29 nM Kd Bioorg Med Chem (2010) 18: 5938-5944 [PMID:20659804]
ChEMBL Binding affinity towards Dopamine receptor D2 B 7.92 pKi 12 nM Ki J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Displacement of [3H]methylspiperone from human low affinity Dopamine D2S receptor by competition binding assay B 7.93 pKi 11.7 nM Ki J Med Chem (2012) 55: 9735-9750 [PMID:23043306]
GtoPdb - - 8.8 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity of compound towards Dopamine receptor D2 using [3H]raclopride (1.2 nM) ligand in striatum bovine was determined B 9.22 pKi 0.6 nM Ki J Med Chem (1997) 40: 952-960 [PMID:9083484]
D2 receptor in Rat [GtoPdb: 215] [UniProtKB: P61169]
GtoPdb - - 7.6 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
ChEMBL Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay B 5.77 pEC50 1700 nM EC50 J Med Chem (2015) 58: 2958-2966 [PMID:25790278]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM B 7.38 pKi 42 nM Ki Bioorg Med Chem Lett (2006) 16: 5303-5308 [PMID:16908150]
ChEMBL Inhibitory concentration against IKr potassium channel B 5.77 pIC50 1700 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG B 7.26 pIC50 54.95 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG channel B 7.26 pIC50 54.6 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 7.26 pIC50 54.6 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 7.3 pIC50 50.12 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 7.3 pIC50 50.12 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory concentration against potassium channel HERG B 7.3 pIC50 50.12 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of hERG K channel F 7.7 pIC50 20 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 7.74 pIC50 18.2 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG in MCF7 cells B 7.74 pIC50 18.2 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibitory activity against Potassium channel HERG B 7.74 pIC50 18 nM IC50 J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 B 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 7.74 pIC50 18 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG channel in HEK293 cells by voltage-clamp method B 8.52 pIC50 3.02 nM IC50 Eur J Med Chem (2008) 43: 2479-2488 [PMID:18262683]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Antagonist activity at H4 receptor (unknown origin) B 5.7 pKi 2000 nM Ki Eur J Med Chem (2017) 125: 565-572 [PMID:27718472]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity against opioid receptor kappa 1 by using [3H]U-69593 as radioligand B 6 pIC50 990 nM IC50 J Med Chem (2001) 44: 3391-3401 [PMID:11585444]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Binding affinity against mu opioid receptor using [3H]DAMGO B 6.43 pIC50 372 nM IC50 J Med Chem (2001) 44: 3391-3401 [PMID:11585444]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.54 pIC50 2900 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 5.54 pIC50 2900 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 6.1 pIC50 800 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.31 pIC50 4900 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 5.31 pIC50 4900 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 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 D10 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 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 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 5.4 pIC50 3981.07 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 5.5 pIC50 3162.28 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 5.6 pIC50 2511.89 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
ChEMBL Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents B 5.74 pIC50 1800 nM IC50 J Med Chem (2016) 59: 5149-5157 [PMID:26588045]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 7.15 pKi 71 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.2 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 9.3 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 9.3 pKi 0.5 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
Nav1.2/Sodium channel protein type II alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775]
ChEMBL Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells B 6.47 pIC50 340 nM IC50 J Med Chem (1996) 39: 1514-1520 [PMID:8691482]
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay B 4.47 pIC50 34200 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795087] [GtoPdb: 2428] [UniProtKB: O94782]
ChEMBL Inhibition of USP1 (unknown origin) assessed as reduction in K63-linked diUb cleavage by gel electrophoresis based orthogonal diUb cleavage assay B 5.7 pIC50 2000 nM IC50 J Med Chem (2015) 58: 1581-1595 [PMID:25364867]
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3]
ChEMBL Inhibition of human USP1/UAF1 complex using Ub-Rho as substrate by qHTS assay B 5.7 pIC50 2000 nM IC50 J Med Chem (2016) 59: 9321-9336 [PMID:27362876]
Cav3.1/Voltage-gated T-type calcium channel alpha-1G subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4641] [GtoPdb: 535] [UniProtKB: O43497]
ChEMBL Inhibition of T-type alpha1G calcium channel B 7.4 pKd 40 nM Kd Bioorg Med Chem Lett (2011) 21: 215-219 [PMID:21126876]
Cav3.1 in Rat [GtoPdb: 535] [UniProtKB: O54898]
GtoPdb - - 7.5 pIC50 - - - J Neurosci (2002) 22: 396-403 [PMID:11784784]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 6.8 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.7 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106]
D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 8.6 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb - - 7.4 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 6.2 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb - - 5.5 pEC50 - - - Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978]
Cav3.2 in Human [GtoPdb: 536] [UniProtKB: O95180]
GtoPdb - - 6.8 pIC50 - - - Eur J Med Chem (2022) 243: 114716 [PMID:36075145]
Cav3.2 in Rat [GtoPdb: 536] [UniProtKB: Q9EQ60]
GtoPdb - - 7.3 pIC50 - - - J Neurosci (2002) 22: 396-403 [PMID:11784784]
Cav3.3 in Human [GtoPdb: 537] [UniProtKB: Q9P0X4]
GtoPdb - - 7.5 pIC50 - - - J Neurosci (2002) 22: 396-403 [PMID:11784784]
Kv1.8 in Human [GtoPdb: 545] [UniProtKB: Q16322]
GtoPdb - - 6.5 pIC50 - - - Am J Physiol Renal Physiol (2000) 278: F1013-21 [PMID:10836990]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]