fascaplysin [Ligand Id: 5969] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL602937 (Fascaplysin)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Non-competitive inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate by Lineweaver-Burk reciprocal plot analysis B 5.64 pKi 2280 nM Ki Medchemcomm (2012) 3: 1098-1103
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate after 30 mins by Ellman's method B 5.83 pIC50 1490 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 4/CDK4/Cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038472] [GtoPdb: 1976] [UniProtKB: P11802, P30281]
ChEMBL Inhibition of CDK4/cyclin-D3 (unknown origin) B 4 pIC50 >100000 nM IC50 Medchemcomm (2012) 3: 1098-1103
GtoPdb CDK4/cyclin D1 complex - 6.46 pIC50 350 nM IC50 Biochem Biophys Res Commun (2000) 275: 877-84 [PMID:10973815]
cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385, Q00534]
ChEMBL Inhibition of CDK6/cyclin-D1 (unknown origin) B 5.47 pIC50 3400 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 6/CDK6/cyclin D2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301386] [GtoPdb: 1978] [UniProtKB: P30279, Q00534]
ChEMBL Inhibition of CDK6/cyclin-D2 (unknown origin) B 4.3 pIC50 >50000 nM IC50 Medchemcomm (2012) 3: 1098-1103
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Non-competitive inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate by Lineweaver-Burk reciprocal plot analysis B 4.31 pKi 48490 nM Ki Medchemcomm (2012) 3: 1098-1103
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate after 30 mins by Ellman's method B 4.04 pIC50 90470 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
ChEMBL Inhibition of CDK1/cyclin-B (unknown origin) B 4 pIC50 >100000 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL Inhibition of CDK2/cyclin-E (unknown origin) B 4.3 pIC50 >50000 nM IC50 Medchemcomm (2012) 3: 1098-1103
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385]
ChEMBL Inhibition of CDK4/cyclin-D1 (unknown origin) B 6.46 pIC50 350 nM IC50 Medchemcomm (2012) 3: 1098-1103
GtoPdb CDK4/cyclin D1 complex - 6.46 pIC50 350 nM IC50 Biochem Biophys Res Commun (2000) 275: 877-84 [PMID:10973815]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301385] [GtoPdb: 1976] [UniProtKB: P11802, P30279]
ChEMBL Inhibition of CDK4/cyclin-D2 (unknown origin) B 4 pIC50 >100000 nM IC50 Medchemcomm (2012) 3: 1098-1103
GtoPdb CDK4/cyclin D1 complex - 6.46 pIC50 350 nM IC50 Biochem Biophys Res Commun (2000) 275: 877-84 [PMID:10973815]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Inhibition of CDK5/p-35 (unknown origin) B 4.7 pIC50 20000 nM IC50 Medchemcomm (2012) 3: 1098-1103

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]