BDBM50378137 Ketek::TELITHROMYCIN

SMILES CC[C@H]1OC(=O)[C@H](C)C(=O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@@](C)(C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCCCn3cnc(c3)-c3cccnc3)C(=O)O[C@]12C)OC

InChI Key InChIKey=LJVAJPDWBABPEJ-PNUFFHFMSA-N

Data  11 IC50  1 EC50

PDB links: 12 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 12 hits for monomerid = 50378137   

TargetSolute carrier organic anion transporter family member 1B3(Homo sapiens (Human))
Ku Leuven

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  5.89E+3nMAssay Description:pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier organic anion transporter family member 1B1(Homo sapiens (Human))
Ku Leuven

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  3.47E+3nMAssay Description:pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  4.00E+4nMAssay Description:Inhibition of human ERG by patch-clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  3.00E+4nMAssay Description:Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  4.00E+3nMAssay Description:Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Homo sapiens (Human))
Ponce De Leon Health

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataEC50:  1.32E+5nMAssay Description:Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A4...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  5.00E+3nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  7.10E+3nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Beijing Institute Of Technology

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  1.18E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes assessed as reduction in metabolite formation using midazolam as substrate incubated for 10 mins in pr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Beijing Institute Of Technology

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50:  1.18E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins after substrate addition by HPLC analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50378137(Ketek | TELITHROMYCIN)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed