clarithromycin [Ligand Id: 10903] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1741 (6-o-methylerythromycin, A-56268, ABBOTT-56268, Biaxin, Biaxin xl, Biaxin Xl Pac, Clarie xl, Clarithromycin, Clarithromycin Extended Release, Clarithromycin identity, Clarosip, Cyllind, Erythromycin, 6-o-methyl-, Febzin xl, Klacid, Klaricid, Klaricid 500, Klaricid adult, Klaricid i.v., Klaricid paed, Klaricid xl, Macladin, Mavid, Mycifor xl, NSC-758704, Prevpac, TE-031, Veclam, Xetinin xl, Zeclar)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
ChEMBL Displacement of [3H]FMZ from GABA-A receptor in rat brain assessed as Kd of [3H]-FMZ at 10 uM after 30 mins by autoradiography (Rvb = 0.66 +/- 0.12 nM) B 9.19 pKd 0.64 nM Kd ACS Med Chem Lett (2016) 7: 746-750 [PMID:27563397]
ChEMBL Displacement of [3H]FMZ from GABA-A receptor in rat brain after 30 mins by autoradiography B 5 pKi >10000 nM Ki ACS Med Chem Lett (2016) 7: 746-750 [PMID:27563397]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 4.23 pIC50 58884.37 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.23 pIC50 58884.37 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 4.23 pIC50 58884.37 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory concentration against IKr potassium channel B 4.34 pIC50 46000 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of K+ channel activity in mammalian cells expressing HERG Kv11.1 B 4.48 pIC50 33113.11 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells F 4.06 pIC50 86700 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells F 4.25 pIC50 56100 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells F 4.3 pIC50 50200 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells F 4.62 pIC50 23800 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 4.82 pIC50 15100 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.14 pIC50 7200 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.42 pIC50 3800 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]

ChEMBL data shown on this page come from version 32:

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]