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: 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 | 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 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]
