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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 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]