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ChEMBL ligand: CHEMBL71752 (Apovincaminic acid ethyl ester, AY-27,255, AY-27255, Bravinton, Cavinton, Ceractin, Ethyl apovincamin-22-oate, NSC-760093, Rgh 4405, Tcv 3b, Ultra-vinca, Vinpocetine, Vinporal) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2017) 60: 3472-3483 [PMID:28406621] |
phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
ChEMBL | Inhibition of PDE10A1 (unknown origin) assessed as decrease in FAM-cAMP hydrolysis after 1 hr by IMAP assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 3472-3483 [PMID:28406621] |
phosphodiesterase 1A/Phosphodiesterase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750] | ||||||||
ChEMBL | Inhibition of PDE1A (unknown origin) | B | 4.72 | pIC50 | 18840 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126472-126472 [PMID:31859156] |
GtoPdb | - | - | 5.1 | pIC50 | 7940 | nM | IC50 | J Biol Chem (1996) 271: 796-806 [PMID:8557689] |
phosphodiesterase 1B/Phosphodiesterase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4425] [GtoPdb: 1295] [UniProtKB: Q01064] | ||||||||
ChEMBL | Inhibition of full length GST-tagged PDE1B (unknown origin) assessed as decrease in FAM-cAMP hydrolysis preincubated for 5 mins followed by FAM-cAMP addition measured after 30 mins by IMAP assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 3472-3483 [PMID:28406621] |
ChEMBL | Inhibition of human recombinant PDE1B using cAMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay | B | 5.1 | pIC50 | 7990 | nM | IC50 | Eur J Med Chem (2021) 209: 112854-112854 [PMID:33022582] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 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 D10 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 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 W2 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 7G8 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 | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
phosphodiesterase 1C in Human [GtoPdb: 1296] [UniProtKB: Q14123] | ||||||||
GtoPdb | - | - | 4.3 | pIC50 | 50100 | nM | IC50 | J Biol Chem (1996) 271: 796-806 [PMID:8557689] |
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]