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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
apelin receptor early endogenous ligand | 442 | None | 0 | Human | Binding | pKd | = | - | 9.29 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/25995451 | |
apelin-13 | 437 | None | 26 | Human | Binding | pKd | = | - | 9.20 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12939143 | |
apelin-13 | 437 | None | 26 | Human | Binding | Ki | = | 0.70 | 9.15 | - | 1 | Displacement of [125I] [NIe75,Tyr77]Pyr-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cells incubated for 1 hr by gamma counting analysis | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.0c01941 | |
apelin-17 | 438 | None | 14 | Human | Binding | Ki | = | 0.04 | 10.40 | - | 1 | Displacement of [125I]-pE13F from human apelin receptor expressed in CHO cell membranes after 1 hr by gamma counting analysis | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm401789v | |
BMS-986224 | 687 | None | 16 | Human | Binding | pKd | = | - | 10.52 | - | 2 | Unclassified | Guide to Pharmacology | 498.1 | 9 | 2 | 9 | 3.99 | CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cn3)o2)c(O)c1-c1c(OC)cccc1OC | https://pubmed.ncbi.nlm.nih.gov/33663236 | |
BMS-986224 | 687 | None | 16 | Human | Binding | Ki | = | 0.07 | 10.13 | - | 2 | Displacement of [3H]Apelin-13 from human APJ receptor stably expressed in human HEK293 cell membrane incubated for 120 mins by TopCount scintillation plate reader analysis | ChEMBL | 498.1 | 9 | 2 | 9 | 3.99 | CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cn3)o2)c(O)c1-c1c(OC)cccc1OC | https://dx.doi.org/10.1021/acs.jmedchem.0c01878 | |
BMS-986224 | 687 | None | 16 | Mouse | Binding | EC50 | = | 0.03 | 10.57 | - | 2 | Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay | ChEMBL | 498.1 | 9 | 2 | 9 | 3.99 | CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cn3)o2)c(O)c1-c1c(OC)cccc1OC | https://dx.doi.org/10.1016/j.bmcl.2021.128325 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | Ki | = | 1.00 | 9.00 | 8 | 2 | Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by Cheng-Prusoff equation analysis | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm501916k | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | IC50 | = | 1.20 | 8.92 | 8 | 2 | Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting method | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm501916k | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 29.00 | 7.54 | 8 | 2 | Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm501916k | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 26.00 | 7.58 | 8 | 2 | Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated for 30 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm501916k | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 0.84 | 9.08 | 8 | 2 | Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm501916k | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | Ki | = | 0.70 | 9.15 | 8 | 2 | Displacement of [125I]-[Nle75, Tyr77] Pyr1-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cell membranes after 1 hr by gamma-counting method | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.7b01353 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 1.10 | 8.96 | 8 | 2 | Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.7b01353 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 60.00 | 7.22 | 8 | 2 | Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.7b01353 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 24.00 | 7.62 | 8 | 2 | Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.7b01353 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | Ki | = | 1.00 | 9.00 | 8 | 2 | Displacement of [125I]-apelin-13 from human APJ receptor stably expressed in CHOK1 cell membrane measured after 2 hrs by topcount scintillation counting method | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1016/j.bmc.2019.115237 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | Ki | = | 0.70 | 9.15 | 8 | 2 | 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 counting based Cheng-Prusoff equation analysis | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.0c01547 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 1.10 | 8.96 | 8 | 2 | Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Galpha(i1)-RlucII(91) assessed as induction of dissociation of Galpha(i1) from G-beta-gamma subunits incubated for 5 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.0c01547 | |
CHEMBL3184840 | 213673 | None | 24 | Human | Binding | EC50 | = | 60.00 | 7.22 | 8 | 2 | Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to APJ incubated for 30 mins by BRET assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/acs.jmedchem.0c01547 |
Showing 1 to 20 of 496 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
[Pyr1]apelin-13 | 3241 | None | 0 | Human | Functional | pIC50 | = | - | 7.90 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11336787 | |
[Pyr1]apelin-13 | 3241 | None | 0 | Human | Functional | pIC50 | = | - | 7.90 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12603839 | |
A77636 | 208 | None | 8 | Human | Functional | IC50 | = | 2779.04 | 5.56 | -912 | 27 | GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR | ChEMBL | 329.2 | 2 | 3 | 4 | 3.25 | NC[C@@H]1O[C@H](C23CC4CC(CC(C4)C2)C3)Cc2c1ccc(O)c2O | https://dx.doi.org/10.6019/CHEMBL5442687 | |
ALX40-4C | 372 | None | 0 | Human | Functional | pIC50 | None | - | 5.50 | -3 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12667811 | |
apelin-13 | 437 | None | 26 | Human | Functional | pIC50 | = | - | 9.15 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10777510 | |
apelin-13 | 437 | None | 26 | Human | Functional | pIC50 | = | - | 9.15 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12603839 | |
apelin-13 | 437 | None | 26 | Human | Functional | pIC50 | = | - | 9.15 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12939143 | |
apelin-13 | 437 | None | 26 | Human | Functional | EC50 | = | 119.43 | 6.92 | - | 1 | GPCR PRESTO-Tango dose-response in agonist mode with target: APLNR | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.6019/CHEMBL5442687 | |
apelin-13 | 437 | None | 26 | Human | Functional | EC50 | = | 0.05 | 10.30 | - | 1 | Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.1c01504 | |
apelin-13 | 437 | None | 26 | Human | Functional | EC50 | = | 40.00 | 7.40 | - | 1 | Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.0c01941 | |
apelin-13 | 437 | None | 26 | Human | Functional | EC50 | = | 43.00 | 7.37 | - | 1 | Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.0c01941 | |
apelin-13 | 437 | None | 26 | Human | Functional | EC50 | = | 1.10 | 8.96 | - | 1 | Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.0c01941 | |
apelin-13 | 437 | None | 26 | Human | Functional | EC50 | = | 0.87 | 9.06 | - | 1 | Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.bmc.2014.04.001 | |
apelin-17 | 438 | None | 14 | Human | Functional | pIC50 | = | - | 8.45 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12603839 | |
apelin-17 | 438 | None | 14 | Human | Functional | pIC50 | = | - | 8.45 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15341513 | |
apelin-17 | 438 | None | 14 | Human | Functional | EC50 | = | 1.90 | 8.72 | - | 1 | Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.ejmech.2019.01.040 | |
apelin-36 | 439 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10777510 | |
apelin-36 | 439 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11336787 | |
apelin-36 | 439 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12603839 | |
apelin-36 | 439 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12939143 |
Showing 1 to 20 of 676 entries