BDBM50241203 CHEMBL414357::HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGSPPPS-NH2::exenatide::exendin-4

SMILES [H][C@](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)([C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@]([H])([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@]([H])([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@@]1([H])C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@@]1([H])C(=O)N1CCC[C@@]1([H])C(=O)N1CCC[C@@]1([H])C(=O)N[C@@H](CO)C(N)=O

InChI Key InChIKey=HTQBXNHDCUEHJF-XWLPCZSASA-N

Data  2 KI  4 IC50  22 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 28 hits for monomerid = 50241203   

TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataKi:  0.0530nMAssay Description:Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataKi:  0.0920nMAssay Description:Displacement of [125I]GLP-1 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Rattus norvegicus)
Sungkyunkwan University

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataIC50:  0.140nMAssay Description:Displacement of [125I]exendin-4 from GLP1 receptor in rat RINm5F cells after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGastric inhibitory polypeptide receptor(Homo sapiens (Human))
Sanofi-Aventis Deutschland

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  200nMAssay Description:Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.000400nMAssay Description:Agonist activity at human GLP1R expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon receptor(Homo sapiens (Human))
Sanofi-Aventis Deutschland

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.000400nMAssay Description:Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon receptor(Mus musculus)
Sanofi-Aventis Deutschland

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Mus musculus)
Sanofi-Aventis Deutschland

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.000500nMAssay Description:Agonist activity at mouse GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon receptor(Homo sapiens (Human))
Sanofi-Aventis Deutschland

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.00180nMAssay Description:Agonist activity at recombinant human GLP1 receptor expressed in HEK293 cells assessed as cAMP accumulation by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.00200nMAssay Description:Activation of human GLP-1 receptor overexpressed in HEK293 cells assessed as cAMP accumulation after 20 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.00600nMAssay Description:Agonist activity at human GLP1 receptor expressed in HEK293 cells assessed as induction of cAMP levels after 20 mins by time-resolved fluorescence an...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.0160nMAssay Description:Agonist activity at human GLP-1R expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataIC50:  6nMAssay Description:Displacement of GLP-1-red from human GLP-1R expressed in CHO-K1 cells by fluorescent competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataIC50:  0.398nMAssay Description:Binding affinity to human GLP-1R expressed in CHO cells coexpressing beta-arrestin-2 incubated for 1 hr by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.000501nMAssay Description:Agonist activity at human GLP-1R expressed in CHO cells coexpressing beta-arrestin-2 assessed as reduction in cAMP accumulation incubated for 2 hrs u...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  794nMAssay Description:Agonist activity at human GLP-1R expressed in CHO cells coexpressing beta-arrestin-2 assessed as stimulation intracellular calcium mobilization measu...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  25nMAssay Description:Agonist activity at human GLP-1R assessed as increase in ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 20 mins by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  50nMAssay Description:Agonist activity at human GLP-1R expressed in CHO cells coexpressing beta-arrestin-2 assessed as increase in beta arrestin-2 recruitment incubated fo...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.0610nMAssay Description:Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins in absence of BETP by plate reader met...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.600nMAssay Description:Agonist activity at FAP-tagged human GLP-1R expressed in HEK293 cells assessed as receptor internalizationMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.110nMAssay Description:Agonist activity at GLP-1R (unknown origin) expressed in candidate selection CHO cells assessed as cAMP accumulation incubated for 30 mins by plate r...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  14nMAssay Description:Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arrestin-1 cell assessed as induction of beta-arrestin 1 recruitment incub...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  9nMAssay Description:Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arrestin-2 cell assessed as induction of beta-arrestin 2 recruitment incub...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.100nMAssay Description:Agonist activity at human GLP-1 receptor expressed in CHO cells assessed as increase in cAMP productionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataEC50:  0.00400nMAssay Description:Agonist activity at human GLP1R expressed in CHO cells assessed as increase in cAMP level by cAMP-response element/luciferase activation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataIC50:  0.660nMAssay Description:Displacement of [125I]GLP1 from human GLP1R expressed in CHOK1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed