BDBM50360601 CHEMBL1933349::MK-0893
SMILES COc1ccc2cc(ccc2c1)-c1cc(nn1[C@@H](C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1cc(Cl)cc(Cl)c1
InChI Key InChIKey=DNTVJEMGHBIUMW-IBGZPJMESA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 23 hits for monomerid = 50360601
Affinity DataKi: 70nMAssay Description:Displacement of [125I]Glucagon-Cex from human GCGRMore data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: 6.60nMAssay Description:Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetGastric inhibitory polypeptide receptor(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 1.02E+3nMAssay Description:Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior ...More data for this Ligand-Target Pair
Affinity DataIC50: 56nMAssay Description:Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 min...More data for this Ligand-Target Pair
TargetUncharacterized protein [173-650](Canis familiaris)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 105nMAssay Description:Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to...More data for this Ligand-Target Pair
Affinity DataIC50: 122nMAssay Description:Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior ...More data for this Ligand-Target Pair
Affinity DataIC50: 727nMAssay Description:Antagonist activity at rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to...More data for this Ligand-Target Pair
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonist activity at human GLP1R expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior...More data for this Ligand-Target Pair
TargetDual specificity protein phosphatase 2(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 9.20E+3nMAssay Description:Antagonist activity at human PAC1 expressed in mouse HIN 3T3 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 m...More data for this Ligand-Target Pair
TargetVasoactive intestinal polypeptide receptor 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 1.16E+4nMAssay Description:Antagonist activity at human VPAC1 expressed in HT-29 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins pri...More data for this Ligand-Target Pair
Affinity DataIC50: 2.43E+4nMAssay Description:This is a review article. Please point to the original journal.More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
Affinity DataIC50: 6.00E+4nMAssay Description:Inhibition of human CYP3A4 in liver microsomes assessed as testosterone 6beta-hydroxylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of human CYP2D6 in liver microsomes assessed as dextromethorphan O-demethylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 2.70E+3nMAssay Description:Inhibition of human CYP2C8 in liver microsomes assessed as paclitaxel 6alpha-hydroxylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 1.40E+4nMAssay Description:Inhibition of human CYP2C9 in liver microsomes assessed as diclofenac 4'-hydroxylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 9.20E+4nMAssay Description:Inhibition of human CYP1A2 in liver microsomes assessed as phenacetin O-deethylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 2.30E+4nMAssay Description:Inhibition of human CYP2B6 in liver microsomes assessed as bupropion hydroxylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of human CYP2E1 in liver microsomes assessed as chlorzoxazone 6beta-hydroxylation after 48 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 80nMAssay Description:Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins ...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting anal...More data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior ...More data for this Ligand-Target Pair
TargetVasoactive intestinal polypeptide receptor 2(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 1.28E+4nMAssay Description:Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior...More data for this Ligand-Target Pair