beta-carboline [Ligand Id: 8222] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275224 (beta-carboline, norharman, norharmane)
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
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  • indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase in Human [ChEMBL: CHEMBL4685] [GtoPdb: 2829] [UniProtKB: P14902]
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  • component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
ChEMBL Inhibitory activity against CKII kinase. B 4.6 pIC50 >25000 nM IC50 Bioorg Med Chem Lett (2003) 13: 2419-2422 [PMID:12824047]
Chitinase in Onchocerca volvulus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795119] [UniProtKB: Q25615]
ChEMBL Inhibition of L3 larval stage of Onchocerca volvulus chitinase using 4-methylumbelliferyl-N-N'-N''-beta-chitotrioside as substrate assessed as release of 4-methylumbelliferone measured for 10 mins by fluorescence assay B 5.07 pIC50 8460 nM IC50 ACS Med Chem Lett (2015) 6: 339-343 [PMID:25815157]
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88]
ChEMBL Inhibition on Benzodiazepine receptor B 5.79 pIC50 1621.81 nM IC50 J Med Chem (1997) 40: 4360-4371 [PMID:9435905]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL In vitro inhibition of [3H]diazepam binding to benzodiazepine receptor in rat cerebral cortical membrane B 5.79 pKi 1620 nM Ki J Med Chem (1982) 25: 1081-1091 [PMID:6127411]
ChEMBL Binding affinity for rat benzodiazepine receptor inverse agonist site B 5.79 pIC50 1621.81 nM IC50 J Med Chem (1996) 39: 2129-2140 [PMID:8667357]
ChEMBL Binding affinity towards benzodiazepine receptor inverse agonist site by the displacement of [3H]diazepam in rat cerebral cortical membranes. B 5.79 pIC50 1621.81 nM IC50 J Med Chem (1993) 36: 2929-2937 [PMID:8411009]
ChEMBL In vitro inhibition of binding to the benzodiazepine receptor in rat cerebral cortical membrane using [3H]diazepam as radioligand B 5.79 pIC50 1620 nM IC50 J Med Chem (1988) 31: 1854-1861 [PMID:2842507]
ChEMBL In vitro inhibition of 3[H]Diazepam binding to Benzodiazepine receptor from rat cerebral cortical membranes B 5.79 pIC50 1620 nM IC50 J Med Chem (1990) 33: 2343-2357 [PMID:2167977]
indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4685] [GtoPdb: 2829] [UniProtKB: P14902]
GtoPdb - - 0.92 pKi 120000000 nM Ki Bioorg Med Chem (2011) 19: 1550-61 [PMID:21269836]
ChEMBL Inhibition of IDO B 6.92 pKi 120 nM Ki Bioorg Med Chem (2011) 19: 1550-1561 [PMID:21269836]
ChEMBL Inhibition of His-tagged recombinant human IDO1 expressed in Escherichia coli using tryptophan as substrate by spectrophotometric analysis B 4.05 pIC50 90000 nM IC50 Bioorg Med Chem (2012) 20: 1354-1363 [PMID:22112538]
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
ChEMBL Inhibitory activity against IkappaB kinase(IKK) isolated from HeLa cells activated with recombinant MEEK1 in an ELISA phosphorylation assay. B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2003) 13: 2419-2422 [PMID:12824047]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL Competitive inhibition of recombinant human MAO-A using kynuramine as substrate by Lineweaver-Burk plot analysis B 6.59 pKi 260 nM Ki Bioorg Med Chem Lett (2018) 28: 2403-2407 [PMID:29925480]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Reversible inhibition of MAO-B B 5.92 pKi 1200 nM Ki Bioorg Med Chem (2011) 19: 7416-7424 [PMID:22071524]
ChEMBL Competitive inhibition of recombinant human MAO-B expressed in baculovirus system using kynuramine as substrate after 40 mins by Lineweaver-Burk plot analysis B 5.95 pKi 1120 nM Ki Bioorg Med Chem Lett (2016) 26: 4714-4719 [PMID:27575476]

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]