BDBM50248106 CHEMBL461101::ELTROMBOPAG::Eltrombopag olamine

SMILES Cc1[nH]n(-c2ccc(C)c(C)c2)c(=O)c1N=Nc1cccc(-c2cccc(c2)C(O)=O)c1O

InChI Key InChIKey=SVOQIEJWJCQGDQ-UHFFFAOYSA-N

Data  4 KI  12 IC50  1 Kd  3 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 20 hits for monomerid = 50248106   

TargetPotassium voltage-gated channel subfamily H member 2(Human)
School of Medicine of University of Electronic Science and Technology of China

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 690nMAssay Description:Inhibition of human ERG channel tail currentMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Sapienza University of Rome

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataKd:  1.32E+4nMAssay Description:Binding affinity to METTL3/METTL14 (unknown origin) assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Sapienza University of Rome

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 4.55E+3nMAssay Description:Inhibition of METTL3/METTL14 (unknown origin) by mass spectrometry-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Sapienza University of Rome

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 3.65E+3nMAssay Description:Inhibition of METTL3/METTL14 (unknown origin) by bioluminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Human)
Federal University of Parana

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 3.10E+3nMAssay Description:Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells membrane vesicles mediated transport of 3[H]-methotrexate for 5 mins using [3H]-methotr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Michigan State University

LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 2.15E+4nMAssay Description:This is a review article. Please point to the original journal.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/27/2022
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Michigan State University

LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataEC50:  8.91E+3nMAssay Description:SARS-CoV-2 CPE assay was conducted at Southern Research Institute (Birmingham, AL) as described in previous reports30, 31. In brief, high ACE2 expres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/21/2020
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Michigan State University

LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 2.15E+4nMAssay Description:The 3CLpro enzyme assay was developed in 384-well black, medium binding microplates (Greiner Bio-One, Monroe, NC, USA) with a total volume of 20 _...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/21/2020
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Michigan State University

LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 8.27E+3nMAssay Description:Ten-point DRCs were generated for each drug. Vero cells were seeded at 1.2 × 104 cells per well in DMEM, supplemented with 2% FBS and 1× ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details Article
PubMed
TargetThrombopoietin receptor(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataEC50:  38nMAssay Description:Agonist activity at human thrombopoietin receptor in Ba/F3 cells assessed as activation of Stat5 response element-driven reporter gene expressionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2012
Entry Details Article
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 1.58E+5nMAssay Description:Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2016
Entry Details Article
PubMed
TargetThrombopoietin receptor(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataEC50:  38nMAssay Description:Agonist activity at human thrombopoietin receptor expressed in mouse Ba/F3 cells by kinase activation based reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 3.16E+5nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
School of Medicine of University of Electronic Science and Technology of China

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 1.58E+6nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonW...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily D member 3(Human)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 1.58E+6nMAssay Description:Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWork...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
School of Medicine of University of Electronic Science and Technology of China

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataIC50: 631nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2016
Entry Details Article
PubMed
TargetSolute carrier organic anion transporter family member 2B1(Human)
Kanazawa University

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataKi:  8.48E+3nMAssay Description:Inhibition of OATP2B1-mediated [3H]estrone-3-sulfate uptake in human OATP2B1 expressing HEK293/PDZK1 cells by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetSolute carrier organic anion transporter family member 1B1(Human)
Kanazawa University

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataKi:  1.49E+4nMAssay Description:Inhibition of OATP1B1-mediated [3H]estrone-3-sulfate uptake in human OATP1B1 expressing HEK293/PDZK1 cells by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetSolute carrier organic anion transporter family member 1B3(Human)
Kanazawa University

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataKi:  2.56E+4nMAssay Description:Inhibition of OATP1B3-mediated [3H]estradiol 17beta-glucuronide uptake in human OATP1B3 expressing HEK293/PDZK1 cells by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetSolute carrier family 22 member 1(Human)
Kanazawa University

Curated by ChEMBL
LigandPNGBDBM50248106(CHEMBL461101 | ELTROMBOPAG | Eltrombopag olamine)
Affinity DataKi:  1.03E+5nMAssay Description:Inhibition of OCT1-mediated [14C]tetraethylammonium uptake in human OCT1 expressing HEK293/PDZK1 cells by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed