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) |
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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 33:
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]
