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 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]
