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

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ChEMBL ligand: CHEMBL532 (Paediathrocin, E-mycin, Erythromycin estolate impurity, free erythromycin-, E-Glades, Erypar, Emgel, Erythro-Statin, Eryacne 2, Erythra-derm, Kerymax, Wyamycin, Sansac, Gallimycin, Pfizer-E, Eryacne 4, J01FA01, Rommix 500 ec, Erymax sprinkle, Zineryt, E-solve 2, A/t/s, NSC-55929, Erythromycin, Benzamycin, E-base, Eryc sprinkles, E-Mycin, Eryc 125, T-stat, Erythro 200, Erycette, Rommix 250 ec, Akne-mycin, Staticin, Bristamycin, Isotrexin, Robimycin, Aknemycin plus, Erygel, R-p mycin, Retcin, Ery-tab, E-glades, Ilotycin, C-solve-2, Stiemycin, Tiloryth, Oftalmolosa cusi eritromicina, Erymax, Erythro-statin, Eryderm, Erythrocin, ERY-TAB, Eryc, PCE, E-Base)
  • Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [UniProtKB: Q06278]
  • This target only has 0 pki data point
  • 0
1 CHEMBL532_lig_chart_1 Aldehyde oxidase Human
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  • CYP1B1/Cytochrome P450 1B1 in Human [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678]
  • This target only has 0 pki data point
  • 0
2 CHEMBL532_lig_chart_2 Cytochrome P450 1B1 Human
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  • GroEL/GroES in Escherichia coli [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1Q7BGE6]
  • This target only has 0 pki data point
  • 0
3 CHEMBL532_lig_chart_3 GroEL/GroES Escherichia coli
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
4 CHEMBL532_lig_chart_4 HERG Human
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5 CHEMBL532_lig_chart_5 HSP60/HSP10 Human
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  • motilin receptor/Motilin receptor in Human [ChEMBL: CHEMBL2203] [GtoPdb: 297] [UniProtKB: O43193]
  • Motilin receptor in Rabbit [ChEMBL: CHEMBL5306] [UniProtKB: A5A4K8]
  • This target only has 1 pki data point
  • 0
6 CHEMBL532_lig_chart_6 Motilin receptor HumanRabbit
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  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
  • This target only has 1 pki data point
  • 0
7 CHEMBL532_lig_chart_7 P-glycoprotein 1 HumanMouse
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  • ABCB1/P-glycoprotein 3 in Mouse [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
  • This target only has 0 pki data point
  • 0
8 CHEMBL532_lig_chart_8 P-glycoprotein 3 Mouse
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
9 CHEMBL532_lig_chart_9 Plasmodium falciparum Plasmodium falciparum
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [UniProtKB: Q06278]
ChEMBL Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis B 4.01 pIC50 96900 nM IC50 WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (null)
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]
GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1Q7BGE6]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
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]
HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809P61604]
ChEMBL Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by malachite green dye based spectrometric analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
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 against Plasmodium falciparum FCR 3TC after 48 hrs F 4.17 pIC50 68000 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity against Plasmodium falciparum FCR 3TC after 48 hrs F 4.17 pIC50 68000 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
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 28:

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]