erythromycin [Ligand Id: 1456] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL532 (Paediathrocin, Erymax Sprinkle, Ery-Tab, E-Glades, Erypar, Emgel, Erythro-Statin, Kerymax, Eryacne 2, Wyamycin, Rommix 250 EC, Sansac, Oftalmolosa Cusi Eritromicina, Gallimycin, C-Solve-2, Pfizer-E, Eryacne 4, E-Solve 2, J01FA01, T-Stat, ERYC, Rommix 500 EC, Zineryt, Eryderm, Erythra-Derm, Akne-Mycin, Erythrocin, Aknemycin Plus, A/T/S, ERY-TAB, NSC-55929, Erythromycin, PCE, Benzamycin, E-Base, E-Mycin, Eryc 125, Erythro 200, Erycette, Staticin, Bristamycin, Isotrexin, R-P Mycin, Robimycin, Erygel, Retcin, Eryc Sprinkles, Ilotycin, Stiemycin, Tiloryth, Erymax)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678]
ChEMBL Inhibition of CYP1B1 (unknown origin) expressed in Escherichia coli DH5alpha coexpressing human NADPH-P450 reductase using 7-Ethoxyresorufin as substrate up to 6 mins in presence of NADP+ by spectrofluorometric analysis B 4.4 pIC50 40000 nM IC50 Eur J Med Chem (2017) 135: 296-306 [PMID:28458135]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory concentration against IKr potassium channel B 4.41 pIC50 39000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG expressed in HEK cells B 7.41 pIC50 39 nM IC50 J. Med. Chem. (2009) 52: 6851-6859 [PMID:19821563]
motilin receptor/Motilin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2203] [GtoPdb: 297] [UniProtKB: O43193]
ChEMBL In vitro binding affinity towards human motilin receptor B 4.43 pKi 37000 nM Ki J. Med. Chem. (2004) 47: 1704-1708 [PMID:15027861]
GtoPdb - - 6.5 pIC50 - - - Science (1999) 284: 2184-8 [PMID:10381885];
J. Pharmacol. Exp. Ther. (2005) 313: 1397-405 [PMID:15764739]
ChEMBL Compound was tested for in vitro motilin receptor binding affinity after treatment with hydrochloric acid solution (pH 2.5) B 7.15 pIC50 70.79 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 835-838
ChEMBL Compound was tested for in vitro motilin receptor binding affinity B 7.36 pIC50 43.65 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 835-838
ChEMBL Agonist activity at motilin receptor F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. (2010) 18: 7651-7658 [PMID:20869254]
ChEMBL Agonist activity at motilin receptor F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 3712-3714 [PMID:21570844]
ChEMBL Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assay F 6.2 pEC50 630.96 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 6429-6436 [PMID:19006669]
ChEMBL In vitro effective concentration towards human motilin receptor F 6.4 pEC50 400 nM EC50 J. Med. Chem. (2004) 47: 1704-1708 [PMID:15027861]
ChEMBL Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay F 7.3 pEC50 50.12 nM EC50 J. Med. Chem. (2009) 52: 1180-1189 [PMID:19191554]
ChEMBL Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay F 7.3 pEC50 50.12 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 6429-6436 [PMID:19006669]
Motilin receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5306] [UniProtKB: A5A4K8]
ChEMBL Agonist activity at motilin receptor in rabbit smooth muscle assessed as maximal possible tissue contraction F 5.92 pEC50 1200 nM EC50 J. Med. Chem. (2009) 52: 6851-6859 [PMID:19821563]
ChEMBL Agonist activity at motilin receptor in rabbit smooth muscle assessed as increase of muscle contraction F 5.92 pEC50 1200 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 5658-5661 [PMID:20801039]
ChEMBL Agonist activity at motilin receptor in rabbit smooth muscle assessed as maximal possible tissue contraction F 5.92 pEC50 1200 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 3712-3714 [PMID:21570844]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells F 4.42 pKi 37790 nM Ki Mol. Pharmacol. (2002) 61: 964-973 [PMID:11961113]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.37 pIC50 43000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.46 pIC50 >35000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.46 pIC50 >35000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.37 pIC50 43000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake F 4.4 pIC50 39500 nM IC50 J. Biol. Chem. (2007) 282: 2494-2504 [PMID:17110371]
ChEMBL Antimalarial activity after 96hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake F 4.46 pIC50 34700 nM IC50 J. Biol. Chem. (2007) 282: 2494-2504 [PMID:17110371]
ChEMBL Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake F 4.69 pIC50 20300 nM IC50 J. Biol. Chem. (2007) 282: 2494-2504 [PMID:17110371]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.74 pIC50 18000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake F 5.03 pIC50 9400 nM IC50 J. Biol. Chem. (2007) 282: 2494-2504 [PMID:17110371]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]