BDBM50014619 CHEMBL3184840

SMILES CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(O)=O

InChI Key InChIKey=GGMAXEWLXWJGSF-PEWBXTNBSA-N

Data  6 KI  1 IC50  2 Kd  28 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 37 hits for monomerid = 50014619   

TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKi:  0.170nMAssay Description:Displacement of [3H]Apelin-13 from human APJ receptor stably expressed in human HEK293 cell membrane incubated for 120 mins by TopCount scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Rattus norvegicus)
University Of Alberta

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKi:  0.300nMAssay Description:Displacement of [125I]-pyr-1-apelin-13 from rat C-terminal EGFP-tagged APJ receptor expressed in CHO cell membranes after 3 hrs by Wallac gamma count...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKi:  0.700nMAssay Description:Binding affinity against sigma receptor from guinea pig brain (minus cerebellum) homogenates, using the novel [3H]-(+/-)-4 as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKi:  0.700nMAssay Description:Displacement of [125I] [NIe75, Tyr77]Pyr-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKi:  1nMAssay Description:Displacement of [125I]-apelin-13 from human APJ receptor stably expressed in CHOK1 cell membrane measured after 2 hrs by topcount scintillation count...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKi:  1nMAssay Description:Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  26nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  5.90nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of GalphaoA subunit dissociation incubated for 5 mins by BRET ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  60nMAssay Description:Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 min...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  24nMAssay Description:Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  1.10nMAssay Description:Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0470nMAssay Description:Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Rattus norvegicus)
University Of Alberta

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0620nMAssay Description:Agonist activity at rat APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  2nMAssay Description:Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilizati...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.300nMAssay Description:Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  1nMAssay Description:Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  54nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-Rh...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  60nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitm...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  1.10nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Galpha(i1)-RlucII(91) assessed as induction of dissociation of Galpha(...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Rattus norvegicus)
University Of Alberta

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  18nMAssay Description:Agonist activity at rat APJ receptor stably expressed in CHO cell membranes in presence of [35S]GTPgammaS by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  3.10nMAssay Description:Agonist activity at human APJ receptor stably expressed in CHO cell membranes in presence of [35S]GTPgammaS by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.300nMAssay Description:Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  1nMAssay Description:Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0500nMAssay Description:Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Rattus norvegicus)
University Of Alberta

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0600nMAssay Description:Agonist activity at rat APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  18nMAssay Description:Agonist activity at human APJ receptor stably expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Mus musculus)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKd:  4.5nMAssay Description:Displacement of [125I]Apelin13 from mouse APJ receptor expressed in HEK293T cells incubated for 1 hr by gamma counter methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0500nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Rattus norvegicus)
University Of Alberta

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0700nMAssay Description:Agonist activity at rat APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataKd:  0.5nMAssay Description:Binding affinity towards human APJ receptor expressed in HEK293 cell membranes and measured by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  29nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataIC50:  1.20nMAssay Description:Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  1.40nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.840nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0500nMAssay Description:Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production a...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.420nMAssay Description:Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50014619(CHEMBL3184840)
Affinity DataEC50:  0.0120nMAssay Description:Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin chall...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed