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ChEMBL ligand: CHEMBL46516 (Fluspirilene, Imap, MCN-JR-6218, R 6218, R-6218, Redeptin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 5.92 | pEC50 | 1200 | 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 | Inhibitory concentration against IKr potassium channel | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906] |
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
ChEMBL | Displacement of [125I]nociceptin from human NOP expressed in CHO cells | B | 6.3 | pKi | 500 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1164-1167 [PMID:19147350] |
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 GB4 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 HB3 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 7G8 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 3D7 after 72 hrs by SYBR green assay | F | 5.7 | pIC50 | 1995.26 | 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 | 5.7 | pIC50 | 1995.26 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting | B | 6.82 | pKi | 151.4 | nM | Ki | J Med Chem (2010) 53: 7573-7586 [PMID:20958049] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting | B | 5.93 | pKi | 1188 | nM | Ki | J Med Chem (2012) 55: 5704-5719 [PMID:22537153] |
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
GtoPdb | - | - | 6 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
GtoPdb | - | - | 5.6 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
GtoPdb | - | - | 8 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
GtoPdb | - | - | 7.9 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
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]