BDBM349662 2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy}pyridin-2-yl)piperidin-1-yl]methyl}-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid::US10208019, Example 1A-09::US10208019, Example 4A-01

SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(C[C@@H]3CCO3)c2c1

InChI Key InChIKey=HYBAKUMPISVZQP-DEOSSOPVSA-N

Data  2 KI  1 IC50  13 EC50

PDB links: 4 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 16 hits for monomerid = 349662   

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

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataKi:  80nMAssay 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
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataKi:  360nMAssay 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
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  1.10nMAssay Description:GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...More data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  13nMAssay Description:GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...More data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  12nMAssay Description:Displacement of [125I]GLP-1 from human GLP-1R (7 to 36 residues) expressed in HEK293 or CHO cell membranes after 120 mins by radioligand binding assa...More data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  0.710nMAssay Description:Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins in presence of BETP by BETP sensitized...More data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  1.10nMAssay 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
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  230nMAssay Description:Agonist activity at FAP-tagged human GLP-1R expressed in HEK293 cells assessed as receptor internalizationMore data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  13nMAssay 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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataIC50:  4.30E+3nMAssay Description:Inhibition of hERG ion channel by patch-clamp methodMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  760nMAssay 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
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  490nMAssay 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
TargetGlucagon-like peptide 1 receptor(Rattus norvegicus)
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50: >2.00E+4nMAssay Description:Activation of rat GLP-1R expressed in CHO cells assessed as increase in cAMP accumulationMore data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Mus musculus)
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50: >2.00E+4nMAssay Description:Activation of mouse GLP-1R expressed in CHO cells assessed as increase in cAMP accumulationMore data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  0.950nMAssay Description:GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...More data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM349662(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Affinity DataEC50:  17nMAssay Description:GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...More data for this Ligand-Target Pair