Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL3559801 npy1r_human Human Yes 10.4 EC50 = 0.0 nM Funct
Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit)
248 2 1 2 3.7 CC(C)(C)c1ccc(OC2CCCCC2O)cc1
CHEMBL4281479 npy1r_human Human Yes 10.0 EC50 = 0.1 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4279973 npy1r_human Human No 9.7 EC50 = 0.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4284905 npy1r_human Human No 9.7 EC50 = 0.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC
CHEMBL4286615 npy1r_human Human No 9.7 EC50 = 0.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O
CHEMBL4279973 npy1r_human Human No 9.7 EC50 = 0.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4284905 npy1r_human Human No 9.7 EC50 = 0.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC
CHEMBL4286615 npy1r_human Human No 9.7 EC50 = 0.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O
CHEMBL3392057 npy1r_human Human Yes 5.0 EC50 = 10072 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
434 2 0 4 6.1 Clc1ccc(-n2c(-c3cccc(Br)c3)nc3nc4ccccc4nc32)cc1
CHEMBL3213459 npy1r_human Human No 5.0 EC50 = 10621 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
443 6 1 6 4.1 O=C(/C(=N/Nc1cccc([N+](=O)[O-])c1)C(=O)C(F)(F)F)c1ccc(Br)cc1
CHEMBL1322039 npy1r_human Human Yes 5.0 EC50 = 10864 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
384 6 2 6 5.3 CCOC(=O)c1nc(Nc2ccc(Nc3ccccc3)cc2)c2ccccc2n1
CHEMBL1311742 npy1r_human Human Yes 5.0 EC50 = 11218 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
497 7 3 6 5.6 O=[N+]([O-])c1cc(C(F)(F)F)cc([N+](=O)[O-])c1NCCN=C(S)Nc1ccc(Cl)c(Cl)c1
CHEMBL1547757 npy1r_human Human Yes 4.9 EC50 = 11573 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
327 3 1 3 3.9 Nc1cc(-c2ccc(Br)cc2)nn1Cc1ccccc1
CHEMBL1538224 npy1r_human Human Yes 4.9 EC50 = 11619 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
317 6 2 3 2.8 OC(CNC1Cc2ccccc2C1)COc1ccc(Cl)cc1
CHEMBL1581332 npy1r_human Human Yes 4.9 EC50 = 11701 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
466 8 3 9 1.7 CCSc1nnc(NC(=O)CCNS(=O)(=O)c2cc(Br)cnc2N)s1
CHEMBL3213319 npy1r_human Human No 4.9 EC50 = 12355 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
273 2 1 4 3.5 Fc1ccc2c(c1)/C(=N/Nc1ccccn1)CCS2
CHEMBL1299267 npy1r_human Human Yes 4.9 EC50 = 12496 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
296 6 1 3 3.5 CCN(CC)CC(O)Cn1c2ccccc2c2ccccc21
CHEMBL4294277 npy1r_human Human No 6.9 EC50 = 125.9 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL1482637 npy1r_human Human Yes 4.9 EC50 = 12619 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
355 4 2 3 4.9 CC(=O)C(=Nc1ccc(Cl)cc1Cl)NNc1cccc(Cl)c1
CHEMBL1602800 npy1r_human Human Yes 4.9 EC50 = 12746 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
551 7 2 5 4.7 O=C(Nc1cc(S(=O)(=O)N2CCCCC2)ccc1Cl)c1ccccc1NS(=O)(=O)c1ccc(F)cc1
CHEMBL4294277 npy1r_human Human No 6.9 EC50 = 130 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL1322039 npy1r_human Human Yes 4.9 EC50 = 13166 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
384 6 2 6 5.3 CCOC(=O)c1nc(Nc2ccc(Nc3ccccc3)cc2)c2ccccc2n1
CHEMBL1329027 npy1r_human Human Yes 4.9 EC50 = 13279 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
431 8 2 5 3.6 CCN(CC)S(=O)(=O)c1ccc2ncc(C(=O)NCCC3=CCCCC3)c(O)c2c1
CHEMBL3099724 npy1r_human Human No 6.9 EC50 = 135 nM Funct
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1519588 npy1r_human Human No 4.9 EC50 = 13550 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
442 6 1 9 3.7 COc1ccc(Nc2oc(/C=C3/SC(=S)N(CC4CCCO4)C3=O)nc2C#N)cc1
CHEMBL2371911 npy1r_human Human No 5.9 EC50 = 1410 nM Funct
Agonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesisAgonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesis
None None None CCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O
CHEMBL3099723 npy1r_human Human No 6.8 EC50 = 144 nM Funct
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)O[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL526034 npy1r_human Human Yes 4.8 EC50 = 14724 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
281 4 1 3 3.8 CN(C)Cc1c(O)ccc2oc(Cc3ccccc3)cc12
CHEMBL1505552 npy1r_human Human Yes 4.8 EC50 = 14783 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
408 7 0 8 3.3 C=CCN1C(=O)/C(=C/c2ccc(OC(C)=O)c(OCC)c2[N+](=O)[O-])SC1=S
CHEMBL4278700 npy1r_human Human No 7.8 EC50 = 15.9 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O
CHEMBL4292105 npy1r_human Human No 7.8 EC50 = 15.9 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL1567983 npy1r_human Human Yes 4.8 EC50 = 15631 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
316 3 2 4 4.2 Oc1ccccc1Cn1c(-c2ccccc2O)nc2ccccc21
CHEMBL1583097 npy1r_human Human Yes 4.8 EC50 = 15697 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
418 6 2 3 4.5 O=C(Cc1ccc(Cl)cc1)Nc1cccc(S(=O)(=O)Nc2ccccc2F)c1
CHEMBL4278700 npy1r_human Human No 7.8 EC50 = 16 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O
CHEMBL4292105 npy1r_human Human No 7.8 EC50 = 16 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL3099724 npy1r_human Human No 6.8 EC50 = 164 nM Funct
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL3192204 npy1r_human Human No 4.8 EC50 = 16470 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
356 10 2 5 4.4 CCCOc1ccc(/C=N/Nc2ccc(C(=O)O)cc2)c(OCCC)c1
CHEMBL3303291 npy1r_human Human No 4.8 EC50 = 16470 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
356 10 2 5 4.4 CCCOc1ccc(/C=N/Nc2ccc(C(=O)O)cc2)c(OCCC)c1
CHEMBL1431189 npy1r_human Human Yes 4.8 EC50 = 16500 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
369 3 2 2 4.2 O=C(CC(O)(C(F)(F)F)C(F)(F)F)Nc1ccc(Cl)c(Cl)c1
CHEMBL1309183 npy1r_human Human Yes 4.8 EC50 = 16732 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
510 6 3 5 4.9 COc1ccc(N=C(S)NC(NC(=O)c2cccc(Cl)c2)C(Cl)(Cl)Cl)c([N+](=O)[O-])c1
CHEMBL1544847 npy1r_human Human Yes 4.8 EC50 = 17105 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
311 2 2 2 4.8 Cc1ccc(Cl)cc1NC(=O)c1cc2ccccc2cc1O
CHEMBL1378687 npy1r_human Human Yes 4.8 EC50 = 17280 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
337 3 2 3 4.5 O=C(Nc1sc2c(c1-c1nc3ccccc3[nH]1)CCCC2)C1CC1
CHEMBL1560379 npy1r_human Human Yes 4.7 EC50 = 18494 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
375 4 0 8 3.1 CCn1nc([N+](=O)[O-])c(C(C#N)c2nc3ccccc3s2)c(Cl)c1=O
CHEMBL1541596 npy1r_human Human Yes 4.7 EC50 = 18547 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
356 6 3 6 3.9 CCCc1cc(-c2[nH]ncc2-c2ccc(C(=O)OCC)o2)c(O)cc1O
CHEMBL1431891 npy1r_human Human Yes 4.7 EC50 = 18569 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
373 4 1 4 3.7 O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1
CHEMBL1537587 npy1r_human Human Yes 4.7 EC50 = 19303 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
359 5 1 5 3.1 COc1ccc(Cn2cnc3c(NS(C)(=O)=O)c(C)c(C)cc32)cc1
CHEMBL439904 npy1r_human Human Yes 5.7 EC50 = 2000 nM Funct
Agonist activity NPY1R (unknown origin) by CRE-luciferase reporter gene assayAgonist activity NPY1R (unknown origin) by CRE-luciferase reporter gene assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1538646 npy1r_human Human Yes 4.7 EC50 = 21818 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
263 5 1 3 2.5 Cc1ccccc1OCC(O)CN1CCC(C)CC1
CHEMBL1623239 npy1r_human Human Yes 4.7 EC50 = 21818 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
263 5 1 3 2.5 Cc1ccccc1OCC(O)CN1CCC(C)CC1
CHEMBL1345141 npy1r_human Human Yes 4.7 EC50 = 22043 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
442 4 1 5 3.6 O=C(O)C1CC=CCC1C(=O)N1CCN(c2nc(-c3ccccc3)c3ccccc3n2)CC1
CHEMBL1517881 npy1r_human Human Yes 4.7 EC50 = 22163 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
452 2 0 7 6.2 Cc1cc2c(cc1C)N(C(=O)CSC1=NCCS1)C(C)(C)c1ssc(=S)c1-2
CHEMBL3099721 npy1r_human Human No 6.7 EC50 = 222 nM Funct
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL2371908 npy1r_human Human No 6.6 EC50 = 240 nM Funct
Agonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesisAgonist activity at human NPY1 receptor in CHO cells by inhibition of forskolin-stimulated cAMP synthesis
None None None CC(C)C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O
CHEMBL1343823 npy1r_human Human Yes 4.6 EC50 = 24380 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
427 5 0 1 7.0 CN(C)c1ccc(-[n+]2c(-c3ccccc3)cc(-c3ccccc3)cc2-c2ccccc2)cc1
CHEMBL1617313 npy1r_human Human Yes 4.6 EC50 = 24380 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
427 5 0 1 7.0 CN(C)c1ccc(-[n+]2c(-c3ccccc3)cc(-c3ccccc3)cc2-c2ccccc2)cc1
CHEMBL1302519 npy1r_human Human Yes 4.6 EC50 = 24391 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
356 3 2 6 5.1 Nc1sc(-c2ccccc2)cc1-c1nnc(S)n1C1CCCCC1
CHEMBL1392858 npy1r_human Human Yes 4.6 EC50 = 26411 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
487 8 2 8 3.5 COC(=O)c1ccc(NC(=O)CSc2nnc(C(C)NC(=O)c3ccccc3Cl)n2C)cc1
CHEMBL1418821 npy1r_human Human No 4.6 EC50 = 26506 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
407 6 2 6 3.4 O=C1C2CC=CCC2C(=O)N1c1ccc(NCCc2ccc(O)cc2)c([N+](=O)[O-])c1
CHEMBL1465891 npy1r_human Human Yes 4.6 EC50 = 27316 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
414 5 4 3 5.1 CCOc1ccc(NC(S)=NN=C(S)Nc2cccc(C(F)(F)F)c2)cc1
CHEMBL1447448 npy1r_human Human Yes 4.5 EC50 = 28902 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
251 2 1 2 4.1 CC(=O)Nc1ccc(-c2cc3ccccc3o2)cc1
CHEMBL1366633 npy1r_human Human Yes 5.5 EC50 = 3068 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
275 1 1 3 3.8 Cc1cccc(N2CCc3c2nc2ccccc2c3N)c1
CHEMBL1454903 npy1r_human Human Yes 5.5 EC50 = 3068 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
275 1 1 3 3.8 Cc1cccc(N2CCc3c2nc2ccccc2c3N)c1
CHEMBL1616892 npy1r_human Human Yes 5.5 EC50 = 3068 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
275 1 1 3 3.8 Cc1cccc(N2CCc3c2nc2ccccc2c3N)c1
CHEMBL4277676 npy1r_human Human No 6.5 EC50 = 316.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4280392 npy1r_human Human No 6.5 EC50 = 316.2 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4277676 npy1r_human Human No 6.5 EC50 = 320 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4280392 npy1r_human Human No 6.5 EC50 = 320 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL1995800 npy1r_human Human Yes 4.5 EC50 = 33309 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
288 4 2 5 2.2 N#C/C(=N/Nc1ccc(OC(F)(F)F)cc1)C(N)=S
CHEMBL1336098 npy1r_human Human Yes 4.5 EC50 = 33757 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
313 5 1 6 2.7 O=C(COc1ccc(Cl)cc1)Nc1ncc([N+](=O)[O-])s1
CHEMBL1549309 npy1r_human Human No 5.5 EC50 = 3408 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
413 2 2 5 5.0 Cc1cccc2c(N)c3c(nc12)CCCC3.O=C(O)c1cc([N+](=O)[O-])ccc1Cl
CHEMBL13 npy1r_human Human Yes 4.5 EC50 = 34827 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O
CHEMBL1504701 npy1r_human Human Yes 4.5 EC50 = 35337 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
464 5 2 6 4.9 O=C(NC(Nc1nc2ccc([N+](=O)[O-])cc2s1)(C(F)(F)F)C(F)(F)F)c1ccccc1
CHEMBL3099722 npy1r_human Human No 6.4 EC50 = 380 nM Funct
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)O[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL439904 npy1r_human Human Yes 8.3 EC50 = 5.6 nM Funct
Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1411397 npy1r_human Human Yes 5.3 EC50 = 5399 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1546 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
368 9 1 4 3.9 CCOC(=O)C(Cc1ccccc1)C(=O)Nc1ccc(N(CC)CC)cc1
CHEMBL1549309 npy1r_human Human No 5.3 EC50 = 5529 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for potentiators or agonists of NPY-Y2: cell-based high-throughput dose response assay for potentiators or agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1539 (Screening assay (NPY-Y2 potentiators or agonists).), 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1791 (Summary AID.)]
413 2 2 5 5.0 Cc1cccc2c(N)c3c(nc12)CCCC3.O=C(O)c1cc([N+](=O)[O-])ccc1Cl
CHEMBL1311742 npy1r_human Human Yes 5.2 EC50 = 5996 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
497 7 3 6 5.6 O=[N+]([O-])c1cc(C(F)(F)F)cc([N+](=O)[O-])c1NCCN=C(S)Nc1ccc(Cl)c(Cl)c1
CHEMBL1519263 npy1r_human Human Yes 5.2 EC50 = 6462 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
293 3 1 4 4.5 Fc1ccc(Nc2c(-c3ccco3)nc3ccccn23)cc1
CHEMBL1373205 npy1r_human Human Yes 5.2 EC50 = 6636 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
220 2 2 3 2.1 Cc1c(C(=O)O)[nH]c2ccc([N+](=O)[O-])cc12
CHEMBL1411397 npy1r_human Human Yes 5.2 EC50 = 7050 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
368 9 1 4 3.9 CCOC(=O)C(Cc1ccccc1)C(=O)Nc1ccc(N(CC)CC)cc1
CHEMBL1573719 npy1r_human Human Yes 5.2 EC50 = 7053 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
174 1 2 5 1.0 N#Cc1c(Cl)nsc1NN
CHEMBL1301994 npy1r_human Human Yes 5.1 EC50 = 7164 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
443 6 2 7 5.2 CCn1c(SCC(=O)Nc2ccc3c(c2)oc2ccccc23)nnc1-c1ccc(N)cc1
CHEMBL1374954 npy1r_human Human Yes 5.1 EC50 = 7410 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
431 5 2 5 5.9 Nc1c(-c2ccccc2)c(CSc2nc3ccccc3[nH]2)nn1-c1ccc(Cl)cc1
CHEMBL1572588 npy1r_human Human Yes 5.1 EC50 = 7410 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
445 4 2 3 4.1 O=C(Nc1ccc(Cl)cc1Cl)NC1CCN(S(=O)(=O)c2ccc(F)cc2)CC1
CHEMBL4277590 npy1r_human Human No 7.1 EC50 = 79 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4277590 npy1r_human Human No 7.1 EC50 = 79.4 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4279794 npy1r_human Human No 6.1 EC50 = 790 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL4279794 npy1r_human Human No 6.1 EC50 = 794.3 nM Funct
Activation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y1R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL1366987 npy1r_human Human Yes 5.1 EC50 = 8195 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
392 2 0 2 6.1 Cc1sc2cc3c(c(C(=O)c4ccccc4)[n+]2c1C)-c1cccc2cccc-3c12
CHEMBL1616832 npy1r_human Human Yes 5.1 EC50 = 8195 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
392 2 0 2 6.1 Cc1sc2cc3c(c(C(=O)c4ccccc4)[n+]2c1C)-c1cccc2cccc-3c12
CHEMBL1548605 npy1r_human Human Yes 5.1 EC50 = 8504 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
366 8 1 4 3.3 C=CCc1ccccc1OCC(O)CN1CCN(c2ccc(C)cc2)CC1
CHEMBL3194195 npy1r_human Human Yes 5.0 EC50 = 9377 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
283 4 1 4 3.5 N#C/C(=N\Nc1ccc(Cl)cc1)C(=O)c1ccccc1
CHEMBL1342462 npy1r_human Human Yes 5.0 EC50 = 9489 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
387 8 1 7 2.2 COc1ccc(N2CCN(CC(O)COc3ccccc3[N+](=O)[O-])CC2)cc1
CHEMBL1618362 npy1r_human Human Yes 5.0 EC50 = 9489 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
387 8 1 7 2.2 COc1ccc(N2CCN(CC(O)COc3ccccc3[N+](=O)[O-])CC2)cc1
CHEMBL13 npy1r_human Human Yes 5.0 EC50 = 9606 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O
CHEMBL1312767 npy1r_human Human Yes 5.0 EC50 = 9709 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high-throughput screening assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1697 (Screening assay (NPY-Y1 agonists).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1704 (Screening assay (CNGC inhibitors).), 1791 (Summary AID.)]
328 4 1 5 3.6 Cn1cc([N+](=O)[O-])c(C(=O)Nc2ccc(C3CCCCC3)cc2)n1
CHEMBL496 npy1r_human Human Yes 5.0 EC50 = 9796 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl
CHEMBL1471202 npy1r_human Human Yes 5.0 EC50 = 9924 nM Funct
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-based high-throughput dose response assay for agonists of NPY-Y1. (Class of assay: confirmatory) [Related pubchem assays: 1703 (Screening assay (CNGC inhibitors).), 1359 (Screening assay (NPY-Y2 potentiators or agonists).), 1304 (Screening assay (NPY-Y1 potentiators or agonists).), 1710 (Screening assay (NPY-Y2 agonists).), 1791 (Summary AID.)]
322 4 1 5 3.3 CC1=NC(=O)C(N=Nc2ccccc2C(=O)O)N1c1ccccc1
CHEMBL269503 npy1r_human Human No 10.7 IC50 = 0.0 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None None
CHEMBL508974 npy1r_human Human No 10.3 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 10.3 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4746035 npy1r_human Human No 10.3 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802520 npy1r_human Human No 10.3 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4786911 npy1r_human Human No 10.2 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
679 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)CBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803593 npy1r_human Human No 10.2 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
679 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)CBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 10.2 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4755692 npy1r_human Human No 10.2 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
629 15 7 5 2.5 CC(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802951 npy1r_human Human No 10.2 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
629 15 7 5 2.5 CC(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL438945 npy1r_human Human Yes 10.2 IC50 = 0.1 nM Bind
Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assayBinding affinity to human neuropeptide Y1 receptor by radioligand displacement assay
None None None None
CHEMBL4794692 npy1r_human Human No 10.1 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803933 npy1r_human Human No 10.1 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4798118 npy1r_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
617 15 8 6 0.8 N/C(=N/C(=O)NCCNC(=O)CO)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4804067 npy1r_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
617 15 8 6 0.8 N/C(=N/C(=O)NCCNC(=O)CO)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL511460 npy1r_human Human No 10.0 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746870 npy1r_human Human No 10.0 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 10.0 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.0 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.0 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 30 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746870 npy1r_human Human No 10.0 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4743858 npy1r_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802419 npy1r_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL511460 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4751322 npy1r_human Human No 9.9 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
655 14 7 5 2.4 N/C(=N/C(=O)NCCNC(=O)C(F)(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802763 npy1r_human Human No 9.9 IC50 = 0.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
655 14 7 5 2.4 N/C(=N/C(=O)NCCNC(=O)C(F)(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 20 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL567112 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
473 9 1 8 5.0 CCc1sc(SCc2cc(N3CCOCC3)cc(NCc3cccc(C)n3)n2)nc1CF
CHEMBL4128926 npy1r_human Human No 9.9 IC50 = 0.1 nM Bind
Displacement of [125I]peptide YY from human Y1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]peptide YY from human Y1 receptor after 120 mins by scintillation counting analysis
583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12
CHEMBL438945 npy1r_human Human Yes 9.9 IC50 = 0.1 nM Bind
Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assayBinding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay
None None None None
CHEMBL3746870 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL585669 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
441 7 1 8 4.8 Cc1cccc(CNc2cc(N3CCSCC3)cc(CSc3nc(C)c(C)o3)n2)n1
CHEMBL3746870 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 9.8 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL267633 npy1r_human Human Yes 9.8 IC50 = 0.2 nM Bind
Displacement of radiolabeled NPY from human neuropeptide Y1 receptorDisplacement of radiolabeled NPY from human neuropeptide Y1 receptor
4251 131 59 59 -18.7 CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CC3=CN=CN3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]6CCCN6C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]7CCCN7C(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]8CCCN8C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]9CCCN9C(=O)[C@H](CC1=CC=C(C=C1)O)N
CHEMBL4753520 npy1r_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
613 15 7 5 2.0 C=CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802860 npy1r_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
613 15 7 5 2.0 C=CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746851 npy1r_human Human No 9.7 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL3747820 npy1r_human Human No 9.7 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL585711 npy1r_human Human No 9.7 IC50 = 0.2 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
459 8 1 8 4.8 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(CF)c(C)s3)n2)n1
CHEMBL438945 npy1r_human Human Yes 9.7 IC50 = 0.2 nM Bind
Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting methodDisplacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method
None None None None
CHEMBL3746851 npy1r_human Human No 9.7 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL3747820 npy1r_human Human No 9.7 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL438945 npy1r_human Human Yes 9.7 IC50 = 0.2 nM Bind
Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 minsDisplacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins
None None None None
CHEMBL511460 npy1r_human Human No 9.6 IC50 = 0.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4745338 npy1r_human Human No 9.6 IC50 = 0.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
627 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)C1CC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802600 npy1r_human Human No 9.6 IC50 = 0.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
627 15 7 5 2.2 N/C(=N/C(=O)NCCNC(=O)C1CC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4762044 npy1r_human Human No 9.6 IC50 = 0.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
641 15 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)C1CCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803174 npy1r_human Human No 9.6 IC50 = 0.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
641 15 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)C1CCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL566020 npy1r_human Human No 9.6 IC50 = 0.3 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
445 7 1 8 4.7 Cc1nc(SCc2cc(N3CCSCC3)cc(NCc3cccc(F)n3)n2)oc1C
CHEMBL566041 npy1r_human Human No 9.6 IC50 = 0.3 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
441 7 1 8 4.6 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)s3)n2)n1
CHEMBL4752935 npy1r_human Human No 9.6 IC50 = 0.3 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
616 15 8 6 0.8 NCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802829 npy1r_human Human No 9.6 IC50 = 0.3 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
616 15 8 6 0.8 NCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746870 npy1r_human Human No 9.5 IC50 = 0.3 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746851 npy1r_human Human No 9.5 IC50 = 0.3 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL3747820 npy1r_human Human No 9.5 IC50 = 0.3 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL567101 npy1r_human Human No 9.4 IC50 = 0.4 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
439 8 1 8 4.4 CCc1oc(SCc2cc(N3CCOCC3)cc(NCc3cccc(C)n3)n2)nc1C
CHEMBL4789673 npy1r_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
693 16 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)CCBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803729 npy1r_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
693 16 7 5 2.6 N/C(=N/C(=O)NCCNC(=O)CCBr)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.4 IC50 = 0.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.4 IC50 = 0.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.4 IC50 = 0.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 9.4 IC50 = 0.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL566040 npy1r_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
451 7 1 8 4.4 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc4c(o3)CCCC4)n2)n1
CHEMBL511460 npy1r_human Human No 9.3 IC50 = 0.5 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746870 npy1r_human Human No 9.3 IC50 = 0.5 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL566255 npy1r_human Human No 9.3 IC50 = 0.6 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
459 8 1 8 4.8 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(CF)s3)n2)n1
CHEMBL4795468 npy1r_human Human No 9.2 IC50 = 0.6 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
649 16 7 5 2.5 N/C(=N/C(=O)NCCNC(=O)CCCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803913 npy1r_human Human No 9.2 IC50 = 0.6 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
649 16 7 5 2.5 N/C(=N/C(=O)NCCNC(=O)CCCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL567719 npy1r_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
425 7 1 8 4.1 Cc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)o3)n2)n1
CHEMBL508974 npy1r_human Human No 9.2 IC50 = 0.7 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.1 IC50 = 0.9 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.1 IC50 = 0.9 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.1 IC50 = 0.9 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746851 npy1r_human Human No 9.1 IC50 = 0.9 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL3747820 npy1r_human Human No 9.1 IC50 = 0.9 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 2 mins by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL267633 npy1r_human Human Yes 9.0 IC50 = 1.0 nM Bind
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
4251 131 59 59 -18.7 CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CC3=CN=CN3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]6CCCN6C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]7CCCN7C(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]8CCCN8C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]9CCCN9C(=O)[C@H](CC1=CC=C(C=C1)O)N
CHEMBL438945 npy1r_human Human Yes 8.9 IC50 = 1.2 nM Bind
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
None None None None
CHEMBL511460 npy1r_human Human No 8.9 IC50 = 1.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL50184 npy1r_human Human No 8.9 IC50 = 1.4 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
557 10 2 8 6.3 CCc1sc(CCc2cc(N3CCOCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL564536 npy1r_human Human Yes 8.9 IC50 = 1.4 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
571 10 2 8 6.8 CCc1sc(CCc2cc(N3CCOCC3)cc(NC(C)c3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL3746870 npy1r_human Human No 8.8 IC50 = 1.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
616 15 6 6 2.7 CCOC(=O)CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL567928 npy1r_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(F)n3)n2)oc1C
CHEMBL3746851 npy1r_human Human No 8.8 IC50 = 1.7 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL3747820 npy1r_human Human No 8.8 IC50 = 1.7 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 1 min by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL566889 npy1r_human Human No 8.8 IC50 = 1.7 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
473 7 1 9 3.5 Cc1cccc(CNc2cc(N3CCS(=O)(=O)CC3)cc(CSc3nc(C)c(C)o3)n2)n1
CHEMBL61532 npy1r_rat Rat No 8.8 IC50 = 1.7 nM Bind
The compound was tested for the binding affinity against Neuropeptide Y receptor type 1 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 1 in rat
524 12 1 6 6.3 Clc1ccc(OCc2nc3c(OCCCN4CCCCC4)cccc3n2CCCC2CCCNC2)cc1
CHEMBL4299523 npy1r_human Human No 8.8 IC50 = 1.8 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells preincubated with radioligand followed by protein addition for 60 mins by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells preincubated with radioligand followed by protein addition for 60 mins by radioligand binding assay
None None None CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@H](C)CC
CHEMBL567941 npy1r_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
443 8 1 8 4.3 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(CF)n3)n2)oc1C
CHEMBL566664 npy1r_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
487 11 1 9 4.3 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(COCCF)n3)n2)oc1C
CHEMBL188790 npy1r_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
585 9 4 9 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3)CC2)NC#N)c1
CHEMBL332347 npy1r_human Human Yes 8.0 IC50 = 10.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL381510 npy1r_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
523 5 1 5 6.2 CC1(F)CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1
CHEMBL417711 npy1r_human Human No 7.0 IC50 = 100 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
525 11 5 3 4.2 N=C(N)NCCCC(NC(=O)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1
CHEMBL17450 npy1r_human Human No 6.0 IC50 = 1000 nM Bind
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
473 13 2 5 7.1 CCCCN(CCCC)CCCNc1nc(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1
CHEMBL42793 npy1r_human Human No 6.0 IC50 = 1000 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
499 10 6 4 3.1 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NC1CCc2cc(O)ccc21
CHEMBL1426022 npy1r_human Human Yes 5.0 IC50 = 10170 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
321 3 1 2 4.3 OC1(c2ccccc2)CCN(Cc2ccccc2)C2CCCCC21
CHEMBL1620460 npy1r_human Human Yes 5.0 IC50 = 10170 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
321 3 1 2 4.3 OC1(c2ccccc2)CCN(Cc2ccccc2)C2CCCCC21
CHEMBL1493277 npy1r_human Human Yes 5.0 IC50 = 10300 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
367 5 1 2 6.1 CC(Sc1ccc(Cl)cc1)C(=O)Nc1ccccc1-c1ccccc1
CHEMBL3194054 npy1r_human Human Yes 5.0 IC50 = 10390 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
538 12 2 7 3.0 COc1ccc(/C=N/NC(=O)CN(CCc2ccccc2)S(=O)(=O)c2ccc(NC(C)=O)cc2)cc1OC
CHEMBL1385608 npy1r_human Human Yes 5.0 IC50 = 10400 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
528 14 0 2 7.7 O=P(CCCCCCCCCP(=O)(c1ccccc1)c1ccccc1)(c1ccccc1)c1ccccc1
CHEMBL2004475 npy1r_human Human No 5.0 IC50 = 10590 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
528 2 3 5 3.8 C/C1=C/[C@@H](C)C/C=C/[C@H]2[C@@H]3O[C@]3(C)[C@@H](C)[C@H]3[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@@]23C(=O)/C=C\C(=O)[C@@H]1O
CHEMBL1426722 npy1r_human Human Yes 5.0 IC50 = 10620 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
403 7 1 5 4.6 Cc1ccc(-n2cc(CNCCn3nc(C)cc3C)c(-c3ccc(F)cc3)n2)cc1
CHEMBL238729 npy1r_human Human No 7.0 IC50 = 107 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
516 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCCNC2)CC1
CHEMBL411800 npy1r_human Human No 6.0 IC50 = 1091 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL264820 npy1r_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
556 11 2 7 7.7 CCc1sc(CCc2cc(OC3CCCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL52282 npy1r_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
542 11 2 7 7.3 CCc1sc(CCc2cc(OC3CCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL392943 npy1r_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
530 5 0 5 6.0 CN1CCC(Cn2c3ccccc3c3cc(C(=O)N4CCN(C)CC4)cc(Oc4ccc(Cl)cc4)c32)CC1
CHEMBL4792205 npy1r_human Human No 7.9 IC50 = 11.5 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
663 15 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803781 npy1r_human Human No 7.9 IC50 = 11.5 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
663 15 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL332347 npy1r_human Human Yes 7.9 IC50 = 11.8 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL441007 npy1r_human Human No 7.0 IC50 = 110 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL289620 npy1r_human Human No 7.0 IC50 = 110 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
457 11 5 3 2.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccccc1
CHEMBL43627 npy1r_human Human No 6.0 IC50 = 1100 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
531 9 4 3 4.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N1CCCc2ccccc2C1
CHEMBL1349920 npy1r_human Human Yes 5.0 IC50 = 11150 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
244 3 0 4 3.2 CCSc1nc2ccc(OC)cc2cc1C#N
CHEMBL1342128 npy1r_human Human Yes 5.0 IC50 = 11350 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
327 4 0 6 3.6 O=C(CSc1nc2ccccc2o1)c1ccc2c(c1)OCCO2
CHEMBL41392 npy1r_human Human No 4.9 IC50 = 11500 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
472 12 5 4 2.3 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccn1
CHEMBL1423382 npy1r_human Human Yes 4.9 IC50 = 11510 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
444 8 0 6 5.4 CCC(Oc1ccc2c(=O)c(-c3ccccc3OC)coc2c1)C(=O)OCc1ccccc1
CHEMBL1456185 npy1r_human Human Yes 4.9 IC50 = 11810 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
254 4 1 4 2.8 C=CCNc1nc(N2CCCC2)nc2ccccc12
CHEMBL290175 npy1r_human Human No 4.9 IC50 = 11900 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1
CHEMBL4281479 npy1r_human Human Yes 7.9 IC50 = 12 nM Funct
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL298983 npy1r_human Human No 7.9 IC50 = 12 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
530 11 2 7 7.2 CCc1sc(CCc2cc(OC(C)C)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL124152 npy1r_human Human No 7.9 IC50 = 12 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
591 10 3 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1
CHEMBL324990 npy1r_human Human No 7.9 IC50 = 12.8 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
606 10 3 8 6.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(S)=N/CCCN2CCC(c3cccc(OC)c3)CC2)c1
CHEMBL2046864 npy1r_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
378 5 0 3 5.3 CCOc1cccc([C@]2(N3CCN(c4ccccc4)CC3)CC[C@@H](C)CC2)c1
CHEMBL166606 npy1r_human Human No 4.9 IC50 = 12000 nM Bind
Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1
513 6 1 6 4.5 COc1ccc2c(c1)CC(NCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2
CHEMBL40475 npy1r_human Human No 4.9 IC50 = 12000 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
565 9 4 3 4.8 N=C(N)NCCCC(NC(=O)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C(=O)N1CCCc2ccccc2C1
CHEMBL240221 npy1r_human Human No 4.9 IC50 = 12022 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
479 5 1 4 5.9 CN(C)C(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F
CHEMBL1383610 npy1r_human Human Yes 4.9 IC50 = 12050 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
308 4 1 6 2.5 Cc1ccc(COC(=O)c2nn(-c3ccccc3)nc2N)cc1
CHEMBL1533962 npy1r_human Human Yes 4.9 IC50 = 12260 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
402 8 1 4 4.5 CCC(C)(C(=O)NC1CCCCC1)N(Cc1ccco1)C(=O)Cc1cccs1
CHEMBL428992 npy1r_human Human No 5.9 IC50 = 1248 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL268409 npy1r_human Human No 5.9 IC50 = 1248 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)O)C(C)C
CHEMBL413232 npy1r_human Human No 5.9 IC50 = 1270 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CN[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)Cc1ccc(O)cc1
CHEMBL1600727 npy1r_human Human Yes 4.9 IC50 = 12770 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
357 5 0 7 5.2 c1ccc(-c2nc(CSc3nnc(-c4cccs4)o3)cs2)cc1
CHEMBL164897 npy1r_human Human No 5.9 IC50 = 1300 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12
CHEMBL2046869 npy1r_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
362 4 0 3 4.4 COc1ccccc1[C@@]1(N2CCN(c3ccccc3)CC2)[C@H]2C[C@H](C)C[C@H]21
CHEMBL562677 npy1r_human Human No 4.9 IC50 = 13000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
374 9 1 7 2.6 CCc1oc(CCc2cc(N3CCOCC3)cc(NCCOC)n2)nc1C
CHEMBL1300782 npy1r_human Human Yes 4.9 IC50 = 13170 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
386 4 0 4 4.5 CCC1=Nc2ccc(Br)cc2C(c2ccccc2)N1CC(=O)OC
CHEMBL203433 npy1r_human Human No 5.9 IC50 = 1318.3 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
534 7 0 6 5.5 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CCCN3CCCCC3)C2=O)CC1
CHEMBL115722 npy1r_human Human No 6.9 IC50 = 132 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
583 9 3 8 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(S)=N/CCCN2CCN(C3CCCCC3)CC2)c1
CHEMBL1359694 npy1r_human Human Yes 4.9 IC50 = 13220 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
294 5 0 4 3.6 CCCCOc1nc2ccccc2c(=O)n1-c1ccccc1
CHEMBL1412538 npy1r_human Human Yes 4.9 IC50 = 13260 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
324 3 3 5 3.4 CCc1cc(-c2[nH]ncc2-c2ccc3c(c2)OCO3)c(O)cc1O
CHEMBL1351633 npy1r_human Human Yes 4.9 IC50 = 13340 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
349 8 1 3 4.1 Cc1cccc(CSCCNC(=O)COc2ccc(Cl)cc2)c1
CHEMBL1439255 npy1r_human Human Yes 4.9 IC50 = 13400 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
327 3 0 6 3.7 Clc1ccc(-c2nnn(Cc3nc4ccccc4s3)n2)cc1
CHEMBL1364371 npy1r_human Human Yes 4.9 IC50 = 13610 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
299 4 0 3 4.3 CN1CCC(Oc2ccccc2Sc2ccccc2)CC1
CHEMBL1616825 npy1r_human Human Yes 4.9 IC50 = 13610 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
299 4 0 3 4.3 CN1CCC(Oc2ccccc2Sc2ccccc2)CC1
CHEMBL1365319 npy1r_human Human Yes 4.9 IC50 = 13630 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
246 5 1 3 2.5 CCCCOc1ccc(C2=NNC(=O)CC2)cc1
CHEMBL1353075 npy1r_human Human Yes 4.9 IC50 = 13680 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
354 9 2 4 2.7 CCCCCCNS(=O)(=O)c1ccc(NC(=O)C2CCCO2)cc1
CHEMBL438923 npy1r_human Human No 5.9 IC50 = 1390 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CN[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C
CHEMBL239568 npy1r_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
601 7 0 6 5.4 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCN(CC(=O)N(C)C)CC2)CC1
CHEMBL189036 npy1r_human Human No 7.9 IC50 = 14 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
653 9 4 9 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3C(F)(F)F)CC2)NC#N)c1
CHEMBL4756494 npy1r_human Human No 7.8 IC50 = 14.5 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
643 14 7 5 2.9 CC(C)(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802928 npy1r_human Human No 7.8 IC50 = 14.5 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
643 14 7 5 2.9 CC(C)(C)C(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL40430 npy1r_human Human No 5.9 IC50 = 1400 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
483 10 5 3 3.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H]1CCc2ccccc21
CHEMBL162093 npy1r_human Human No 4.9 IC50 = 14000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
521 9 2 5 4.4 COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL1391119 npy1r_human Human No 4.8 IC50 = 14700 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
352 8 2 5 3.3 CCCCNC(=O)c1onc(CSc2ccccc2F)c1C(=O)O
CHEMBL1771260 npy1r_human Human No 7.8 IC50 = 15 nM Funct
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
477 8 2 7 4.9 CCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1
CHEMBL41673 npy1r_human Human No 6.8 IC50 = 150 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1
CHEMBL159450 npy1r_human Human No 4.8 IC50 = 15000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
536 9 2 6 4.3 O=[N+]([O-])c1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL560382 npy1r_human Human No 4.8 IC50 = 15000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
375 6 1 8 3.2 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)sc1C
CHEMBL562831 npy1r_human Human No 4.8 IC50 = 15000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
402 9 1 8 2.5 CCOC(=O)CNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1
CHEMBL1550184 npy1r_human Human Yes 4.8 IC50 = 15070 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
289 1 0 1 3.9 CC1CC(C)CN(C2=CC(=[N+]3CCCC3)CC(C)(C)C2)C1
CHEMBL1624501 npy1r_human Human Yes 4.8 IC50 = 15070 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
289 1 0 1 3.9 CC1CC(C)CN(C2=CC(=[N+]3CCCC3)CC(C)(C)C2)C1
CHEMBL214707 npy1r_human Human No 5.8 IC50 = 1514 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1989 63 30 26 -7.7 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL412257 npy1r_human Human No 5.8 IC50 = 1567 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1989 66 30 26 -7.3 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O
CHEMBL378587 npy1r_human Human No 4.8 IC50 = 15848.9 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
521 7 0 6 5.6 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCOCC1
CHEMBL266021 npy1r_human Human No 5.8 IC50 = 1586 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O
CHEMBL410792 npy1r_human Human No 6.8 IC50 = 159 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL217692 npy1r_human Human No 5.8 IC50 = 1597 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CN[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL48950 npy1r_human Human No 7.8 IC50 = 16 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
544 13 2 7 7.6 CCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL411795 npy1r_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
516 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2CCNCC2)CC1
CHEMBL332347 npy1r_human Human Yes 7.8 IC50 = 16.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL4764296 npy1r_human Human No 7.8 IC50 = 16.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
681 15 7 5 3.3 N/C(=N/C(=O)NCCNC(=O)c1ccc(F)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803298 npy1r_human Human No 7.8 IC50 = 16.2 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
681 15 7 5 3.3 N/C(=N/C(=O)NCCNC(=O)c1ccc(F)cc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL564513 npy1r_human Human No 4.8 IC50 = 16000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
344 7 1 6 3.0 CCNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1
CHEMBL1504083 npy1r_human Human Yes 4.8 IC50 = 16710 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
375 7 0 4 4.6 CCOC(=O)C1(CCCc2ccccc2)CCN(C2CCSCC2)CC1
CHEMBL1555711 npy1r_human Human No 4.8 IC50 = 16800 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
368 8 2 5 3.8 CCCCNC(=O)c1onc(CSc2ccc(Cl)cc2)c1C(=O)O
CHEMBL383763 npy1r_human Human No 6.8 IC50 = 169.8 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCN(C)C[C@@H]3F)C2=O)CC1
CHEMBL299598 npy1r_human Human No 7.8 IC50 = 17 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
530 12 2 7 7.2 CCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL52325 npy1r_human Human No 7.8 IC50 = 17 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
556 12 2 7 7.6 CCc1sc(CCc2cc(OCC3(C)CC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL44246 npy1r_human Human Yes 7.8 IC50 = 17 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL2046861 npy1r_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
348 3 1 3 4.1 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccc(O)cc1)N1CCN(c2ccccc2)CC1
CHEMBL41457 npy1r_human Human No 6.8 IC50 = 170 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1
CHEMBL165556 npy1r_human Human No 4.8 IC50 = 17000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
551 10 2 6 4.4 COc1cc2c(cc1OC)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL116864 npy1r_human Human No 6.8 IC50 = 176 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
567 9 3 8 4.6 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCN(C3CCCCC3)CC2)c1
CHEMBL2046863 npy1r_human Human No 6.8 IC50 = 180 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
350 3 0 2 4.5 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccc(F)cc1)N1CCN(c2ccccc2)CC1
CHEMBL162094 npy1r_human Human No 4.8 IC50 = 18000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
505 8 2 4 4.7 Cc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL411200 npy1r_human Human No 6.7 IC50 = 183 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O
CHEMBL41981 npy1r_human Human No 6.7 IC50 = 184 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1
CHEMBL395640 npy1r_human Human No 6.7 IC50 = 186 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
574 6 0 5 6.5 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C3CC3)C[C@@H]2F)CC1
CHEMBL382355 npy1r_human Human No 6.7 IC50 = 186.2 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
524 5 1 6 4.6 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@@H]3CCNC[C@@H]3F)C2=O)CC1
CHEMBL240038 npy1r_human Human No 5.7 IC50 = 1862 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
562 8 2 5 6.4 CN1CCCC1CCNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F
CHEMBL426314 npy1r_human Human No 5.7 IC50 = 1862.1 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
527 5 1 5 6.1 O=C1c2c(n(CC3CCNCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCC(F)(F)CC1
CHEMBL1545205 npy1r_human Human Yes 4.7 IC50 = 18900 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
323 4 1 3 4.5 CC(C)(C)NC(=O)c1oc2ccccc2c1COc1ccccc1
CHEMBL3198593 npy1r_human Human No 4.7 IC50 = 18920 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
377 7 1 7 3.9 CCOC(=O)C(/C=N/c1cc(C)nn1-c1ccc(Cl)cc1)=C(\O)OCC
CHEMBL568152 npy1r_human Human No 7.7 IC50 = 19 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
473 10 1 9 4.2 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccc(OCCF)n3)n2)oc1C
CHEMBL288355 npy1r_human Human No 7.7 IC50 = 19 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1
CHEMBL2046858 npy1r_human Human No 6.7 IC50 = 190 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
347 3 1 3 4.0 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1cccc(N)c1)N1CCN(c2ccccc2)CC1
CHEMBL167318 npy1r_human Human No 4.7 IC50 = 19000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
521 9 2 5 4.4 COc1ccc2c(c1)CC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL392583 npy1r_human Human No 5.7 IC50 = 1905 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
557 5 1 6 6.0 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCn2ccnc2C1
CHEMBL240208 npy1r_human Human No 6.7 IC50 = 191 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
536 8 1 5 5.8 CN(C)CCN(C)C(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F
CHEMBL1350415 npy1r_human Human Yes 4.7 IC50 = 19100 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
412 5 1 4 5.1 CC(C)OC(=O)/C(=C/c1ccc2c(c1)c1ccccc1n2C)NC(=O)c1ccccc1
CHEMBL1538792 npy1r_human Human Yes 5.7 IC50 = 1938 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
440 7 1 7 4.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2ccc(O)c(CN3CCOCC3)c12
CHEMBL187555 npy1r_human Human No 8.7 IC50 = 2 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
591 10 4 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3OC)CC2)c1
CHEMBL188271 npy1r_human Human No 8.7 IC50 = 2 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
561 9 4 8 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3)CC2)c1
CHEMBL366340 npy1r_human Human No 8.7 IC50 = 2 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
606 10 4 10 4.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3[N+](=O)[O-])CC2)c1
CHEMBL446342 npy1r_human Human No 8.7 IC50 = 2.2 nM Bind
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL470495 npy1r_human Human No 8.7 IC50 = 2.2 nM Bind
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 8.6 IC50 = 2.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 8.6 IC50 = 2.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 8.6 IC50 = 2.4 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL438945 npy1r_human Human Yes 8.6 IC50 = 2.6 nM Bind
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
None None None None
CHEMBL438411 npy1r_human Human No 8.6 IC50 = 2.7 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None None
CHEMBL508974 npy1r_human Human No 8.6 IC50 = 2.8 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL49177 npy1r_human Human No 7.7 IC50 = 20 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
606 14 2 7 8.4 CCc1sc(CCc2cc(OCCCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL41673 npy1r_human Human No 6.7 IC50 = 200 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1
CHEMBL1341841 npy1r_human Human Yes 4.7 IC50 = 20260 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
457 5 1 6 4.6 Cc1ccc(-c2nn3c(C)nnc3c3ccccc23)cc1S(=O)(=O)NC(C)c1ccccc1
CHEMBL1771261 npy1r_human Human No 6.7 IC50 = 207 nM Funct
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
491 9 2 7 5.3 CCCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1
CHEMBL582790 npy1r_human Human No 7.7 IC50 = 21 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3ccc(F)nc3)n2)oc1C
CHEMBL551197 npy1r_human Human No 4.7 IC50 = 21000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
373 7 1 8 3.0 CCc1oc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)nc1C
CHEMBL556183 npy1r_human Human No 4.7 IC50 = 21000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
355 7 1 7 2.5 CCc1oc(CCc2cc(N3CCOCC3)cc(NCC#N)n2)nc1C
CHEMBL296523 npy1r_human Human No 4.7 IC50 = 21000 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
483 10 5 3 3.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H]1CCc2ccccc21
CHEMBL1511420 npy1r_human Human Yes 4.7 IC50 = 21010 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
442 5 2 7 2.8 COc1ccc(NC(=O)c2nnc(O)c3ccccc23)cc1S(=O)(=O)N1CCCCC1
CHEMBL41166 npy1r_human Human No 4.7 IC50 = 21800 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
457 11 5 3 3.0 N=C(N)NCCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)NCc1ccccc1
CHEMBL382836 npy1r_human Human No 7.7 IC50 = 22.4 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
505 5 1 5 6.1 CC1CCN([C@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1
CHEMBL2046868 npy1r_human Human No 5.7 IC50 = 2200 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
332 3 0 2 4.4 C[C@H]1C[C@H]2[C@@H](C1)[C@]2(c1ccccc1)N1CCN(c2ccccc2)CC1
CHEMBL43710 npy1r_human Human No 5.7 IC50 = 2200 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
497 9 4 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2ccccc2C1
CHEMBL351082 npy1r_human Human No 4.7 IC50 = 22000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
507 10 2 5 3.8 COc1ccc2c(c1)CC(CNCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2
CHEMBL560921 npy1r_human Human No 4.7 IC50 = 22000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
369 8 1 7 2.9 CCc1oc(CCc2cc(N3CCOCC3)cc(NCCC#N)n2)nc1C
CHEMBL290175 npy1r_human Human No 4.7 IC50 = 22000 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1
CHEMBL43753 npy1r_human Human No 4.7 IC50 = 22300 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CO)c1ccccc1
CHEMBL1608455 npy1r_human Human Yes 4.6 IC50 = 22650 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
470 9 1 9 4.1 COc1ccccc1CN(Cc1cc2cc(C)ccc2nc1O)Cc1nnnn1Cc1ccco1
CHEMBL432237 npy1r_human Human No 6.6 IC50 = 231 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
565 8 3 9 4.7 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(N/C(=N/CCCN2CCC(C(C)(C)C)CC2)NC#N)c1
CHEMBL411637 npy1r_human Human No 6.6 IC50 = 233 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL49795 npy1r_human Human No 6.6 IC50 = 234 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
502 10 2 7 6.4 CCc1sc(CCc2cc(OC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL4436741 npy1r_human Human No 6.6 IC50 = 234.4 nM Bind
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
1735 55 28 24 -2.7 COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)OC
CHEMBL45869 npy1r_human Human No 6.6 IC50 = 237 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
578 12 2 7 8.0 CCc1sc(CCc2cc(OCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL379443 npy1r_human Human No 6.6 IC50 = 239.9 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
524 5 1 6 4.6 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@H]3CCNC[C@@H]3F)C2=O)CC1
CHEMBL42686 npy1r_human Human No 5.6 IC50 = 2400 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1
CHEMBL187902 npy1r_human Human No 7.6 IC50 = 25 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
645 10 4 9 5.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3OC(F)(F)F)CC2)c1
CHEMBL412698 npy1r_human Human No 6.6 IC50 = 250 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL433627 npy1r_human Human No 5.6 IC50 = 2500 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
471 11 4 3 3.2 C[C@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1
CHEMBL557648 npy1r_human Human No 4.6 IC50 = 25000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
358 7 1 6 3.4 CCc1oc(CCc2cc(N3CCOCC3)cc(NC(C)C)n2)nc1C
CHEMBL440944 npy1r_human Human No 4.6 IC50 = 25118.9 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
423 3 0 5 4.2 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C)C2=O)CC1
CHEMBL430274 npy1r_human Human No 6.6 IC50 = 257 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccsc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL268351 npy1r_human Human No 4.6 IC50 = 26000 nM Bind
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C1CCCCC1)C1CCCCC1
CHEMBL428915 npy1r_human Human No 6.6 IC50 = 263 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
562 8 2 5 6.4 CCN1CCCC1CNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F
CHEMBL2397200 npy1r_human Human No 6.6 IC50 = 265 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cnccn4)CC3)C3CC(C)CC32)c1
CHEMBL3213775 npy1r_human Human Yes 4.6 IC50 = 26730 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
334 7 1 6 2.1 CCCCC(=O)N/N=C/c1ccc(N2CCOCC2)c([N+](=O)[O-])c1
CHEMBL1319576 npy1r_human Human Yes 4.6 IC50 = 26740 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
286 0 1 3 4.4 Nc1c2c(nc3sc4c(c13)CCCC4)CCCCCC2
CHEMBL114040 npy1r_human Human No 6.6 IC50 = 268 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
585 9 3 9 4.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(N/C(=N/CCCN2CCC(c3ccccc3)CC2)NC#N)c1
CHEMBL4751466 npy1r_human Human No 7.6 IC50 = 27 nM Funct
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
5195 171 80 72 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)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@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL405527 npy1r_human Human No 6.6 IC50 = 275 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL412378 npy1r_human Human No 6.6 IC50 = 279 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL238517 npy1r_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
548 5 0 5 5.9 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C)C[C@@H]2F)CC1
CHEMBL187782 npy1r_human Human No 7.6 IC50 = 28 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
669 10 4 10 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3OC(F)(F)F)CC2)NC#N)c1
CHEMBL540466 npy1r_human Human No 6.6 IC50 = 280 nM Funct
Antagonist activity at human neuropeptide Y1 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAntagonist activity at human neuropeptide Y1 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
581 8 1 4 6.0 COc1ccc([C@H](N[C@@H]2CC[C@@H](C(=O)N3CCC(C(=O)N4CCCC4)(c4ccccc4)CC3)C(C)(C)C2)C(F)F)cc1
CHEMBL42747 npy1r_human Human No 6.6 IC50 = 280 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1
CHEMBL164971 npy1r_human Human No 5.6 IC50 = 2800 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL239775 npy1r_human Human No 5.5 IC50 = 2882 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
557 5 2 5 6.1 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCc2[nH]cnc2C1
CHEMBL49461 npy1r_human Human No 7.5 IC50 = 29 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
570 11 2 7 8.1 CCc1sc(CCc2cc(OC3CCCCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL351508 npy1r_human Human No 4.5 IC50 = 29000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
521 9 2 5 4.4 COc1ccc2c(c1)CC(CNC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL187399 npy1r_human Human No 8.5 IC50 = 3 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
586 9 4 9 4.4 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3C#N)CC2)c1
CHEMBL187925 npy1r_human Human No 8.5 IC50 = 3 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
631 10 4 10 4.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3SC)CC2)NC#N)c1
CHEMBL189412 npy1r_human Human No 8.5 IC50 = 3 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
610 9 4 10 4.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3C#N)CC2)NC#N)c1
CHEMBL267633 npy1r_human Human Yes 8.5 IC50 = 3.1 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
4251 131 59 59 -18.7 CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CC3=CN=CN3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]6CCCN6C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]7CCCN7C(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]8CCCN8C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]9CCCN9C(=O)[C@H](CC1=CC=C(C=C1)O)N
CHEMBL332347 npy1r_human Human Yes 8.4 IC50 = 3.6 nM Bind
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL332347 npy1r_human Human Yes 8.4 IC50 = 4.0 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cellsDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL48897 npy1r_human Human No 7.5 IC50 = 30 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
592 13 2 7 8.0 CCc1sc(CCc2cc(OCCc3ccccc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL4751668 npy1r_human Human No 7.5 IC50 = 30.9 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
669 15 7 5 3.4 N/C(=N/C(=O)NCCNC(=O)C1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802795 npy1r_human Human No 7.5 IC50 = 30.9 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
669 15 7 5 3.4 N/C(=N/C(=O)NCCNC(=O)C1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL2046870 npy1r_human Human No 6.5 IC50 = 300 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
362 4 0 3 4.4 COc1cccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)c1
CHEMBL41686 npy1r_human Human No 5.5 IC50 = 3000 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21
CHEMBL1562842 npy1r_human Human Yes 4.5 IC50 = 30390 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
412 6 1 4 4.6 COc1ccccc1N(CC(=O)NC1CCCC1)C(=O)c1oc(C(C)(C)C)cc1C
CHEMBL187492 npy1r_human Human No 7.5 IC50 = 31 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
629 9 4 8 5.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3C(F)(F)F)CC2)c1
CHEMBL1376342 npy1r_human Human Yes 4.5 IC50 = 31850 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
289 4 1 2 4.9 O=C(O)c1ccc(N(c2ccccc2)c2ccccc2)cc1
CHEMBL571013 npy1r_human Human No 4.5 IC50 = 32000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
330 6 1 6 2.6 CCc1oc(CCc2cc(N3CCOCC3)cc(NC)n2)nc1C
CHEMBL1307319 npy1r_human Human Yes 5.5 IC50 = 3205 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
420 5 0 7 4.3 CCN(C(=O)c1ccc(C(C)(C)C)cc1)c1nnc(Cn2nnc3ccccc32)s1
CHEMBL1609697 npy1r_human Human Yes 4.5 IC50 = 32170 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
479 7 1 8 3.5 O=C(NC1CCCCC1)C(c1ccncc1)N(Cc1ccc2c(c1)OCO2)C(=O)c1cnsn1
CHEMBL48947 npy1r_human Human No 7.5 IC50 = 33 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
516 11 2 7 6.8 CCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL424862 npy1r_human Human No 7.5 IC50 = 33.9 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
520 5 0 6 5.0 CN1CCC(Cn2c3c(c4ccccc42)C(=O)C(N2CCN(C)CC2)C[C@H]3Oc2ccc(Cl)cc2)CC1
CHEMBL206799 npy1r_human Human No 6.5 IC50 = 331.1 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
520 7 1 6 5.2 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCNCC1
CHEMBL204583 npy1r_human Human No 5.5 IC50 = 3388.4 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
519 7 0 5 6.7 O=C1c2c(n(CCCN3CCCCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCCCC1
CHEMBL1312220 npy1r_human Human Yes 5.5 IC50 = 3391 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
351 5 2 3 4.1 Cc1cc2cc(C)c(NCCNC(=O)c3cccc(F)c3)nc2cc1C
CHEMBL48456 npy1r_human Human No 7.5 IC50 = 35 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
558 14 2 7 8.0 CCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL266077 npy1r_human Human No 4.5 IC50 = 35000 nM Bind
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC
CHEMBL165506 npy1r_human Human No 4.5 IC50 = 35000 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
507 8 2 5 4.1 COc1ccc2c(c1)CC(NC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL4456247 npy1r_human Human No 6.4 IC50 = 363.1 nM Bind
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O
CHEMBL1381600 npy1r_human Human Yes 5.4 IC50 = 3648 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
351 2 0 1 5.1 Cc1ccc(-[n+]2c(-c3ccccc3)cn3c2CCc2ccccc2-3)c(C)c1
CHEMBL1619019 npy1r_human Human Yes 5.4 IC50 = 3648 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
351 2 0 1 5.1 Cc1ccc(-[n+]2c(-c3ccccc3)cn3c2CCc2ccccc2-3)c(C)c1
CHEMBL380654 npy1r_human Human No 7.4 IC50 = 37.2 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
536 7 2 7 4.0 O=C1c2c(n(CC3CCNCC3)c3ccccc23)[C@H](Oc2ccc(Cl)cc2)CC1N1CCN(CCO)CC1
CHEMBL43628 npy1r_human Human No 5.4 IC50 = 3750 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
458 11 5 4 2.3 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccccn1
CHEMBL549699 npy1r_human Human No 4.4 IC50 = 38000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
372 6 1 8 2.5 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)n(C)c1C
CHEMBL203430 npy1r_human Human No 5.4 IC50 = 3890.5 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
520 5 1 6 4.1 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1=O
CHEMBL414482 npy1r_human Human No 7.4 IC50 = 39 nM Bind
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C1CCCCC1
CHEMBL189548 npy1r_human Human No 7.4 IC50 = 39 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
615 10 3 10 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCCN2CCN(c3cccc(OC)c3)CC2)NC#N)c1
CHEMBL60737 npy1r_human Human No 7.4 IC50 = 39 nM Bind
The compound was tested for the binding affinity against Neuropeptide Y receptor type 1The compound was tested for the binding affinity against Neuropeptide Y receptor type 1
408 7 0 4 5.3 CC[C@H]1CC[C@@](c2cccc(OCOC)c2)(N2CCN(c3ccccc3)CC2)CC1
CHEMBL410938 npy1r_human Human No 6.4 IC50 = 398 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL187491 npy1r_human Human No 8.4 IC50 = 4 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
575 9 4 8 4.8 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3C)CC2)c1
CHEMBL187620 npy1r_human Human No 8.4 IC50 = 4 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
615 10 4 10 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3OC)CC2)NC#N)c1
CHEMBL188576 npy1r_human Human No 8.4 IC50 = 4 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
630 10 4 11 4.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3[N+](=O)[O-])CC2)NC#N)c1
CHEMBL361273 npy1r_human Human No 8.4 IC50 = 4 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
599 9 4 9 4.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3C)CC2)NC#N)c1
CHEMBL324554 npy1r_human Human No 8.4 IC50 = 4.2 nM Bind
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cellsBinding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
590 10 3 8 5.5 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCCN2CCC(c3cccc(OC)c3)CC2)c1
CHEMBL3746851 npy1r_human Human No 8.4 IC50 = 4.3 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL3747820 npy1r_human Human No 8.4 IC50 = 4.3 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis
611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1
CHEMBL566663 npy1r_human Human No 8.4 IC50 = 4.3 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
455 9 1 9 4.0 COCc1cccc(CNc2cc(N3CCOCC3)cc(CSc3nc(C)c(C)o3)n2)n1
CHEMBL52108 npy1r_human Human No 8.4 IC50 = 4.4 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
572 11 2 8 7.0 CCc1sc(CCc2cc(OC3CCOCC3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL2113710 npy1r_human Human No 8.3 IC50 = 4.7 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
570 14 2 7 8.2 CC/C=C\CCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL437027 npy1r_human Human Yes 8.3 IC50 = 4.7 nM Bind
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cellsDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells
None None None None
CHEMBL1345334 npy1r_human Human Yes 5.4 IC50 = 4021 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
340 5 0 3 5.3 COc1ccc(Cn2c(/C=C/c3ccccc3)nc3ccccc32)cc1
CHEMBL1428935 npy1r_human Human Yes 5.4 IC50 = 4079 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
373 4 0 5 4.8 N#CC(C#N)=C1C=CC=CN1/C(=C\c1ccco1)C(=O)c1ccc(Cl)cc1
CHEMBL1353428 npy1r_human Human Yes 5.4 IC50 = 4084 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
377 4 0 4 4.6 Cc1cccc(-n2ccnc2SCC(=O)N2CCCc3ccccc32)c1C
CHEMBL4749279 npy1r_human Human No 7.4 IC50 = 41 nM Funct
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
5221 175 80 73 -23.1 CC[C@H](C)[C@H](NC(=O)C(Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)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@@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL2397201 npy1r_human Human No 7.4 IC50 = 42 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
377 5 0 4 4.2 CCOc1cccc(C2(N3CCN(c4ccccn4)CC3)C3CC(C)CC32)c1
CHEMBL1402158 npy1r_human Human Yes 5.4 IC50 = 4261 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
366 5 0 3 5.1 Cc1ccccc1/C=C/c1nc2ccccc2c(=O)n1CCc1ccccc1
CHEMBL2397293 npy1r_human Human No 5.4 IC50 = 4270 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
379 5 0 6 3.0 CCOc1cccc(C2(N3CCN(c4ncncn4)CC3)C3CC(C)CC32)c1
CHEMBL438342 npy1r_human Human No 7.4 IC50 = 43 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
532 5 1 5 5.8 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CC2=C(F)CNCC2)CC1
CHEMBL560182 npy1r_human Human No 5.4 IC50 = 4300 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
398 7 1 6 3.5 CCc1oc(CCc2cc(N3CCOCC3)cc(NCC(F)(F)F)n2)nc1C
CHEMBL331578 npy1r_human Human No 6.4 IC50 = 434 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
568 9 3 9 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(NC(=O)NCCCN2CCN(C3CCCCC3)CC2)c1
CHEMBL382204 npy1r_human Human No 6.4 IC50 = 436.5 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
538 5 0 6 4.9 CN1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3C[C@H]3CCN(C)C[C@@H]3F)C2=O)CC1
CHEMBL1312713 npy1r_human Human Yes 5.4 IC50 = 4368 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
394 9 1 5 4.2 CCN(CC)CC(O)COc1ccc2c(c1)c(C(C)=O)c(C)n2-c1ccccc1
CHEMBL2397294 npy1r_human Human No 5.4 IC50 = 4380 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cccnn4)CC3)C3CC(C)CC32)c1
CHEMBL1502859 npy1r_human Human Yes 5.4 IC50 = 4380 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
375 4 1 7 2.1 O=c1c2ccccc2nc2c3ccccc3c(NCCN3CCOCC3)nn12
CHEMBL415176 npy1r_human Human No 4.4 IC50 = 44000 nM Bind
Compound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cellsCompound was evaluated for its inhibitory activity against human neuropeptide Y1 receptor expressing SK-N-MC cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C1CCCCC1
CHEMBL1580409 npy1r_human Human Yes 5.4 IC50 = 4465 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
429 4 1 4 5.3 CN1CCN(c2ccccc2NC(=O)c2ccc(-c3ccc(Cl)cc3Cl)o2)CC1
CHEMBL262221 npy1r_human Human No 6.4 IC50 = 447 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)C(c1ccccc1)c1ccccc1
CHEMBL417727 npy1r_human Human Yes 5.3 IC50 = 4542 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
223 0 1 3 2.3 Nc1ccc2c(c1)C(=O)C(=O)c1ccccc1-2
CHEMBL4750988 npy1r_human Human No 6.3 IC50 = 457.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
683 16 7 5 3.8 N/C(=N/C(=O)NCCNC(=O)CC1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802711 npy1r_human Human No 6.3 IC50 = 457.1 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
683 16 7 5 3.8 N/C(=N/C(=O)NCCNC(=O)CC1CCCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL1531745 npy1r_human Human Yes 5.3 IC50 = 4576 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
437 8 1 5 4.7 COc1cccc(-c2ccc(C#N)c(SCC(=O)NCCc3ccc(Cl)cc3)n2)c1
CHEMBL2046860 npy1r_human Human No 6.3 IC50 = 460 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
346 3 0 2 4.7 Cc1ccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)cc1
CHEMBL42686 npy1r_human Human No 5.3 IC50 = 4600 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1
CHEMBL238736 npy1r_human Human No 6.3 IC50 = 467 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
548 6 1 5 6.0 CN(C)C1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@H]2F)C1
CHEMBL2111764 npy1r_human Human No 7.3 IC50 = 47.9 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL427594 npy1r_human Human No 7.3 IC50 = 48.9 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL439506 npy1r_human Human No 7.3 IC50 = 49.0 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
506 5 1 6 4.6 CN1CCN([C@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1
CHEMBL1419096 npy1r_human Human Yes 5.3 IC50 = 4826 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
392 5 2 9 2.1 COC(=O)c1ccccc1NC(=O)Cn1c(-c2nonc2N)nc2ccccc21
CHEMBL1471779 npy1r_human Human Yes 5.3 IC50 = 4838 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
500 5 0 7 5.1 COC(=O)c1c(C)oc2ccc(N(C(=O)c3ccncc3)S(=O)(=O)c3ccc4ccccc4c3)cc12
CHEMBL4445077 npy1r_human Human No 6.3 IC50 = 489.8 nM Bind
Agonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging methodAgonist activity at GFP-tagged neuropeptide Y1R (unknown origin) expressed in HEK293T cells assessed as beta-arrestin2 recruitment measured after 60 mins by H33342 staining-based imaging method
1703 54 30 22 -4.3 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)C/C=C\C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O
CHEMBL362083 npy1r_human Human No 8.3 IC50 = 5 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
607 10 4 9 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3SC)CC2)c1
CHEMBL364380 npy1r_human Human No 8.3 IC50 = 5 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
601 9 5 10 3.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3ccccc3O)CC2)NC#N)c1
CHEMBL584908 npy1r_human Human No 8.3 IC50 = 5.2 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3ccnc(F)c3)n2)oc1C
CHEMBL113935 npy1r_human Human No 8.3 IC50 = 5.4 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
584 9 3 8 5.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCCN2CCC(c3ccccc3)CC2)NC#N)c1
CHEMBL51284 npy1r_human Human No 8.3 IC50 = 5.5 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
558 13 2 7 8.0 CCc1sc(CCc2cc(OC(CC)CC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL44246 npy1r_human Human Yes 8.2 IC50 = 5.9 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL239773 npy1r_human Human No 7.3 IC50 = 50 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
544 7 0 5 6.5 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3CCCN2CCCCC2)CC1
CHEMBL398782 npy1r_human Human No 7.3 IC50 = 50 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
522 8 2 5 5.5 CN(C)CCNC(=O)c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F
CHEMBL1499276 npy1r_human Human Yes 5.3 IC50 = 5010 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
396 3 1 4 5.2 Cc1ccc(-c2cc(C(=O)Nc3ccc4c(c3)OCCO4)c3ccccc3n2)cc1
CHEMBL3211272 npy1r_human Human Yes 5.3 IC50 = 5022 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
317 5 2 2 3.4 S=C(NCCc1ccccc1)N/N=C/c1ccccc1Cl
CHEMBL2397296 npy1r_human Human No 5.3 IC50 = 5032 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4cncnc4)CC3)C3CC(C)CC32)c1
CHEMBL240404 npy1r_human Human No 7.3 IC50 = 51 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
534 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@@H]2F)CC1
CHEMBL1468302 npy1r_human Human Yes 5.3 IC50 = 5100 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
414 5 1 5 5.3 Nn1c(Cc2cccc3ccccc23)nnc1SCc1c(Cl)cccc1Cl
CHEMBL42861 npy1r_human Human No 4.3 IC50 = 51000 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
573 10 4 3 4.7 N=C(N)NCCCC(NC(=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N1CCCc2ccccc2C1
CHEMBL1585445 npy1r_human Human Yes 5.3 IC50 = 5137 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
330 5 0 5 4.3 COc1ccc(-c2noc(COc3ccc(Cl)c(C)c3)n2)cc1
CHEMBL1201049 npy1r_human Human Yes 5.3 IC50 = 5146 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL808 npy1r_human Human Yes 5.3 IC50 = 5146 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL1457093 npy1r_human Human Yes 5.3 IC50 = 5161 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
346 8 2 3 4.0 O=C(COc1ccccc1CNCc1ccccc1)Nc1ccccc1
CHEMBL1621407 npy1r_human Human Yes 5.3 IC50 = 5161 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
346 8 2 3 4.0 O=C(COc1ccccc1CNCc1ccccc1)Nc1ccccc1
CHEMBL1559259 npy1r_human Human Yes 5.3 IC50 = 5210 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
392 5 0 7 4.1 COC(=O)c1ccc(CSc2nc3ccccc3c(=O)n2-c2ccccc2)o1
CHEMBL4746354 npy1r_human Human No 6.3 IC50 = 524.8 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
753 17 7 5 4.7 N/C(=N/C(=O)NCCNC(=O)C(c1ccccc1)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802592 npy1r_human Human No 6.3 IC50 = 524.8 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
753 17 7 5 4.7 N/C(=N/C(=O)NCCNC(=O)C(c1ccccc1)c1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL1427745 npy1r_human Human No 5.3 IC50 = 5265 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
405 7 1 4 3.5 CCC(NCCC(c1ccccc1)c1ccccc1)=C1C(=O)N(C)C(=O)N(C)C1=O
CHEMBL1522356 npy1r_human Human Yes 5.3 IC50 = 5266 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
372 3 0 3 5.8 Clc1ccc(CSc2cc3c(nn2)-c2ccccc2CC3)cc1Cl
CHEMBL392787 npy1r_human Human No 7.3 IC50 = 53 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
534 5 1 5 5.6 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCNC[C@H]2F)CC1
CHEMBL41686 npy1r_human Human No 5.3 IC50 = 5300 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21
CHEMBL1312703 npy1r_human Human Yes 5.3 IC50 = 5306 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
375 4 1 4 4.7 COC(=O)c1cc(Cl)c(NC(=O)c2ccc(C(C)(C)C)cc2)cc1OC
CHEMBL3195229 npy1r_human Human Yes 5.3 IC50 = 5335 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
398 6 1 4 4.4 O=C(N/N=C/c1ccco1)c1ccccc1OCc1ccc(Br)cc1
CHEMBL1308845 npy1r_human Human Yes 5.3 IC50 = 5388 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
367 7 1 2 5.0 Cc1cc(Cl)c(OCCCNCc2ccccc2)c(Br)c1
CHEMBL1616638 npy1r_human Human Yes 5.3 IC50 = 5388 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
367 7 1 2 5.0 Cc1cc(Cl)c(OCCCNCc2ccccc2)c(Br)c1
CHEMBL2397291 npy1r_human Human No 7.3 IC50 = 54 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
378 5 0 5 3.6 CCOc1cccc(C2(N3CCN(c4ncccn4)CC3)C3CC(C)CC32)c1
CHEMBL1537995 npy1r_human Human Yes 5.3 IC50 = 5404 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
359 5 0 4 5.7 Cc1nc(-c2ccccc2)sc1C(=O)CSc1ccc(Cl)cc1
CHEMBL1568243 npy1r_human Human Yes 5.3 IC50 = 5470 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
259 3 0 2 4.1 O=C(/C=C/c1cccc2ccccc12)c1ccncc1
CHEMBL422583 npy1r_human Human No 7.3 IC50 = 55 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
558 11 2 7 7.8 CCc1sc(CCc2cc(OCC(C)(C)C)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL2046862 npy1r_human Human No 6.3 IC50 = 550 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
362 4 0 3 4.4 COc1ccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)cc1
CHEMBL1431004 npy1r_human Human Yes 5.3 IC50 = 5537 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
388 8 0 7 3.8 CCOc1nc(SCCOc2ccc(Cl)cc2Cl)nc(N(C)C)n1
CHEMBL116230 npy1r_human Human No 6.3 IC50 = 554 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
591 10 3 9 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(NC(=O)NCCCN2CCC(c3cccc(OC)c3)CC2)c1
CHEMBL1348426 npy1r_human Human Yes 5.3 IC50 = 5546 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
363 7 0 5 3.6 CC(C)COc1ccc(C(=O)OC2CC(C)(C)OCC2CN(C)C)cc1
CHEMBL1617044 npy1r_human Human Yes 5.3 IC50 = 5546 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
363 7 0 5 3.6 CC(C)COc1ccc(C(=O)OC2CC(C)(C)OCC2CN(C)C)cc1
CHEMBL1487131 npy1r_human Human Yes 5.3 IC50 = 5680 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
335 4 0 6 4.1 CC(C)c1ccc(-c2nnn(Cc3nc4ccccc4s3)n2)cc1
CHEMBL1423799 npy1r_human Human Yes 5.3 IC50 = 5687 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
371 4 0 4 5.6 N#Cc1ccc(-c2cccnc2)nc1SCc1ccc(Cl)c(Cl)c1
CHEMBL1427504 npy1r_human Human Yes 5.3 IC50 = 5687 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
401 6 1 2 6.5 O=C(CSCc1c(Cl)cccc1Cl)Nc1ccccc1-c1ccccc1
CHEMBL1453672 npy1r_human Human Yes 5.2 IC50 = 5724 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
407 6 1 3 5.8 O=C(COC(=O)c1ccc(-c2ccccc2)cc1)Nc1ccccc1-c1ccccc1
CHEMBL1493500 npy1r_human Human Yes 5.2 IC50 = 5769 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
444 7 1 5 5.9 CCc1cccc(CC)c1NC(=O)COC(=O)c1ccccc1-c1nc2ccccc2s1
CHEMBL1426896 npy1r_human Human Yes 5.2 IC50 = 5853 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
426 5 0 7 4.4 C/C=C(/C)C(=O)O[C@@H]1c2c(ccc3ccc(=O)oc23)O[C@@H]1C(C)(C)OC(=O)/C(C)=C\C
CHEMBL360205 npy1r_human Human No 8.2 IC50 = 6 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
577 9 5 9 4.2 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3ccccc3O)CC2)c1
CHEMBL51290 npy1r_human Human No 8.2 IC50 = 6.5 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
607 14 2 8 7.8 CCc1sc(CCc2cc(OCCCc3cccnc3)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL288355 npy1r_human Human No 7.2 IC50 = 60 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1
CHEMBL18016 npy1r_human Human No 4.2 IC50 = 60000 nM Bind
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
419 4 1 7 2.9 COc1cc2nc(N3CCC(N4Cc5ccccc5C4=O)CC3)nc(N)c2cc1OC
CHEMBL1310577 npy1r_human Human Yes 5.2 IC50 = 6031 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
293 4 0 2 5.1 CN(C)Cc1ccccc1Sc1cccc2ccccc12
CHEMBL1616775 npy1r_human Human Yes 5.2 IC50 = 6031 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
293 4 0 2 5.1 CN(C)Cc1ccccc1Sc1cccc2ccccc12
CHEMBL1452153 npy1r_human Human Yes 5.2 IC50 = 6057 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
345 4 0 2 4.4 Cc1ccc(C(=O)C[n+]2cc(-c3ccccc3)n3c2CCCCC3)cc1
CHEMBL1621027 npy1r_human Human Yes 5.2 IC50 = 6057 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
345 4 0 2 4.4 Cc1ccc(C(=O)C[n+]2cc(-c3ccccc3)n3c2CCCCC3)cc1
CHEMBL1335124 npy1r_human Human Yes 5.2 IC50 = 6127 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
391 6 1 3 5.2 O=C(COC(=O)/C=C/c1ccc(Cl)cc1)Nc1ccccc1-c1ccccc1
CHEMBL2397299 npy1r_human Human No 7.2 IC50 = 62 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
376 5 0 3 4.8 CCOc1cccc(C2(N3CCN(c4ccccc4)CC3)C3CC(C)CC32)c1
CHEMBL2046867 npy1r_human Human No 7.2 IC50 = 62 nM Bind
Displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation countingDisplacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells after 1 hr by scintillation counting
376 5 0 3 4.8 CCOc1cccc([C@@]2(N3CCN(c4ccccc4)CC3)[C@H]3C[C@H](C)C[C@H]32)c1
CHEMBL51422 npy1r_human Human No 7.2 IC50 = 63 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
572 15 2 7 8.4 CCCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL1379143 npy1r_human Human Yes 5.2 IC50 = 6324 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
422 6 2 4 4.8 Cc1cccc(N=C(S)N(CCN(C)C)Cc2cc3cc(C)cc(C)c3nc2O)c1
CHEMBL1393538 npy1r_human Human Yes 5.2 IC50 = 6433 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
458 8 1 5 3.6 Cc1ccccc1C(=O)c1cccn1CC(=O)NCCN1CCN(c2cccc(C)c2C)CC1
CHEMBL206671 npy1r_human Human No 6.2 IC50 = 645.7 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
533 7 0 5 7.0 CC1CCN(C2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CCCN3CCCCC3)C2=O)CC1
CHEMBL3190644 npy1r_human Human Yes 5.2 IC50 = 6459 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
295 3 1 4 3.7 CC(C)COC(=O)c1cccc2c1-c1ccccc1/C2=N\O
CHEMBL1327690 npy1r_human Human Yes 5.2 IC50 = 6664 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
331 4 0 5 4.2 N#Cc1nc(COc2ccc(Cl)cc2)oc1N1CCCCCC1
CHEMBL1336318 npy1r_human Human Yes 5.2 IC50 = 6687 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
335 4 0 3 5.2 O=C(c1ccco1)c1cn(Cc2ccc(Cl)cc2)c2ccccc12
CHEMBL42747 npy1r_human Human No 6.2 IC50 = 670 nM Bind
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 1 in SK-N-MC cells
513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1
CHEMBL425095 npy1r_human Human No 6.2 IC50 = 674 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1407634 npy1r_human Human Yes 5.2 IC50 = 6748 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
446 4 0 4 5.6 Cc1c(OCc2c(F)cccc2Cl)c(=O)ccn1-c1ncc(C(F)(F)F)cc1Cl
CHEMBL1414494 npy1r_human Human Yes 5.2 IC50 = 6837 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
326 3 1 2 4.4 CC1=CC(C)(C)N(C(=O)CNC2CCCCC2)c2cc(C)ccc21
CHEMBL1620238 npy1r_human Human Yes 5.2 IC50 = 6837 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
326 3 1 2 4.4 CC1=CC(C)(C)N(C(=O)CNC2CCCCC2)c2cc(C)ccc21
CHEMBL1446166 npy1r_human Human Yes 5.2 IC50 = 6943 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
314 3 1 3 4.7 O=C(Nc1ccc(Cl)cc1)c1csc(-c2ccccc2)n1
CHEMBL1574689 npy1r_human Human Yes 5.2 IC50 = 6952 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
390 4 0 8 3.5 COC(=O)c1ccc(CSc2nc3sc4c(c3c(=O)n2C)CCCC4)o1
CHEMBL1610409 npy1r_human Human Yes 5.2 IC50 = 6959 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
328 5 0 4 5.2 Clc1ccccc1CSc1nnc(/C=C/c2ccccc2)o1
CHEMBL1462215 npy1r_human Human Yes 5.2 IC50 = 6978 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
365 3 0 3 5.5 CC[n+]1c(/C=C2\SC(c3ccccc3C)=CN2C)sc2ccccc21
CHEMBL1621471 npy1r_human Human Yes 5.2 IC50 = 6978 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
365 3 0 3 5.5 CC[n+]1c(/C=C2\SC(c3ccccc3C)=CN2C)sc2ccccc21
CHEMBL1771259 npy1r_human Human Yes 8.2 IC50 = 7 nM Funct
Antagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assayAntagonist activity at NPY Y1 receptor in human SK-N-MC cells assessed as inhibition of NPY-induced calcium mobilization by FLIPR assay
463 7 2 7 4.5 COc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1
CHEMBL4755079 npy1r_human Human No 8.1 IC50 = 7.6 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
655 15 7 5 3.0 N/C(=N/C(=O)NCCNC(=O)C1CCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802896 npy1r_human Human No 8.1 IC50 = 7.6 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
655 15 7 5 3.0 N/C(=N/C(=O)NCCNC(=O)C1CCCC1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 8.1 IC50 = 7.6 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 8.1 IC50 = 7.6 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 8.1 IC50 = 7.6 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL567708 npy1r_human Human No 8.1 IC50 = 7.7 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
429 7 1 8 4.0 Cc1nc(SCc2cc(N3CCOCC3)cc(NCc3cccnc3F)n2)oc1C
CHEMBL563011 npy1r_human Human No 4.2 IC50 = 70000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
359 6 1 8 2.8 Cc1nc(SCc2cc(N3CCOCC3)cc(NCC#N)n2)oc1C
CHEMBL3208997 npy1r_human Human Yes 5.2 IC50 = 7083 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
322 6 0 6 3.1 COc1cc(/C=N/n2cnnc2)ccc1OCc1ccc(C)cc1
CHEMBL1990096 npy1r_human Human Yes 5.2 IC50 = 7084 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
325 5 0 4 4.7 C/C(=N\OC(=O)c1ccc(OC(C)C)cc1)c1ccc(C)c(C)c1
CHEMBL1328939 npy1r_human Human Yes 5.2 IC50 = 7100 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
434 3 1 5 5.6 Cc1nc(N2CCCCC2)c2c(C)c(C(=O)Nc3ccccc3C(F)(F)F)sc2n1
CHEMBL1545971 npy1r_human Human Yes 5.2 IC50 = 7125 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
383 3 1 5 5.0 Cc1onc(-c2ccccc2Cl)c1C(=O)Nc1sc2c(c1C#N)CCC2
CHEMBL1480648 npy1r_human Human Yes 5.1 IC50 = 7156 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
415 4 1 7 3.4 COc1ccc(-n2nc(C(=O)Nc3ccc4c(c3)OCO4)c3ccccc3c2=O)cc1
CHEMBL48493 npy1r_human Human No 7.1 IC50 = 72 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
586 16 2 7 8.8 CCCCCCCOc1cc(CCc2nc(C)c(CC)s2)nc(NCc2cc(Cl)cc(NC(=O)OC(C)C)c2)c1
CHEMBL1308461 npy1r_human Human Yes 5.1 IC50 = 7229 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
281 1 0 4 3.9 Cc1nc(N2CCC(C)CC2)c2oc3ccccc3c2n1
CHEMBL206112 npy1r_human Human No 5.1 IC50 = 7244.4 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
436 6 0 4 6.3 O=C1CC[C@@H](Oc2ccc(Cl)cc2)c2c1c1ccccc1n2CCCN1CCCCC1
CHEMBL564979 npy1r_human Human Yes 5.1 IC50 = 7273 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
394 6 1 4 5.5 Cc1ccc(CCC(=O)Nc2ncc(Cc3cc(Cl)ccc3Cl)s2)o1
CHEMBL1386511 npy1r_human Human Yes 5.1 IC50 = 7326 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
313 6 0 4 3.7 CN(C)CCCSc1nc(-c2ccccc2)nc2c1CCC2
CHEMBL428292 npy1r_human Human No 6.1 IC50 = 735 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@H](CN[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C
CHEMBL1457690 npy1r_human Human Yes 5.1 IC50 = 7359 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
387 3 0 2 5.2 COc1ccc(-[n+]2c(-c3ccc(Cl)cc3)cn3c2CCc2ccccc2-3)cc1
CHEMBL1621585 npy1r_human Human Yes 5.1 IC50 = 7359 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
387 3 0 2 5.2 COc1ccc(-[n+]2c(-c3ccc(Cl)cc3)cn3c2CCc2ccccc2-3)cc1
CHEMBL1383592 npy1r_human Human Yes 5.1 IC50 = 7387 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
346 5 2 3 3.1 Cc1ccc(NC(=O)C(=O)NCCOc2ccc(Cl)cc2)c(C)c1
CHEMBL2314835 npy1r_human Human No 7.1 IC50 = 74 nM Bind
Binding affinity to Y1 receptor in human SK-N-MC cellsBinding affinity to Y1 receptor in human SK-N-MC cells
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)[C@H](CCCCNC(=O)COCC(=O)NCCOCCOCC(=O)NCC(=O)Nc1ccc(C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)cc1)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O
CHEMBL1458887 npy1r_human Human Yes 5.1 IC50 = 7428 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
325 4 1 2 4.7 CC(C)(C)NCc1cc(Br)ccc1OC1CCCC1
CHEMBL1621543 npy1r_human Human Yes 5.1 IC50 = 7428 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
325 4 1 2 4.7 CC(C)(C)NCc1cc(Br)ccc1OC1CCCC1
CHEMBL1311570 npy1r_human Human Yes 5.1 IC50 = 7444 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
426 6 0 6 5.0 C1=CC=NC(=C1)C2=NN=C(N2CC3=CC=CO3)SCC4=CC=C(C=C4)Br
CHEMBL43523 npy1r_human Human No 5.1 IC50 = 7500 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
500 12 6 4 1.9 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(N)=O)c1ccccc1
CHEMBL428320 npy1r_human Human No 7.1 IC50 = 77.0 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL42625 npy1r_human Human No 4.1 IC50 = 76000 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
497 9 4 3 3.6 N=C(N)NCCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2ccccc2C1
CHEMBL438935 npy1r_human Human No 6.1 IC50 = 762 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1539256 npy1r_human Human Yes 5.1 IC50 = 7623 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
496 10 1 8 4.0 COc1ccc(NC(=O)CSc2nc3ccccc3c(=O)n2CCCN2CCCCC2)c(OC)c1
CHEMBL1329549 npy1r_human Human Yes 5.1 IC50 = 7628 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
496 11 2 10 4.6 CCOC(=O)CCCCC(=O)c1[nH]c(O)nc1CSc1nnc2c3ccccc3n(C(C)C)c2n1
CHEMBL413612 npy1r_human Human No 6.1 IC50 = 764 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1366620 npy1r_human Human Yes 5.1 IC50 = 7662 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
342 5 2 2 4.2 CCCCCC(=O)NC(=S)Nc1ccc(Br)cc1C
CHEMBL1389982 npy1r_human Human Yes 5.1 IC50 = 7683 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
311 1 1 2 5.2 Oc1cccc(-c2nc3ccc4ccccc4c3c3c2CCC3)c1
CHEMBL441936 npy1r_human Human No 6.1 IC50 = 769 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
1916 63 29 26 -8.4 CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CN[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)CC(C)C
CHEMBL1599610 npy1r_human Human Yes 5.1 IC50 = 7697 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
282 3 1 2 4.1 O=C(/C=C/c1cccc(Cl)c1)c1nc2ccccc2[nH]1
CHEMBL1342925 npy1r_human Human Yes 5.1 IC50 = 7704 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
370 4 0 6 4.7 COC(=O)c1cc2occc2n1Cc1nc(-c2ccccc2Cl)oc1C
CHEMBL206723 npy1r_human Human No 6.1 IC50 = 776.3 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
506 5 1 6 4.6 CN1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1
CHEMBL238527 npy1r_human Human No 5.1 IC50 = 7762 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
535 5 2 5 5.8 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCC(O)CC1
CHEMBL1439981 npy1r_human Human Yes 5.1 IC50 = 7767 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
349 6 1 6 4.4 COc1ccc(-c2nc(C#N)c(NC(C)c3ccccc3)o2)cc1OC
CHEMBL1570844 npy1r_human Human Yes 5.1 IC50 = 7799 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
441 6 1 5 4.9 COc1ccc(-c2[nH]nc3c2C(c2ccc(OC)c(OC)c2)N(c2ccccc2)C3=O)cc1
CHEMBL1468490 npy1r_human Human Yes 5.1 IC50 = 7817 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
331 2 0 3 2.6 O=C1C2CC=C(Cl)CC2C(=O)N1CC1Cc2ccccc2CO1
CHEMBL262083 npy1r_human Human Yes 5.1 IC50 = 7826 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
343 4 4 9 0.2 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccccc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL511460 npy1r_human Human No 8.1 IC50 = 8 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL566441 npy1r_human Human No 8.1 IC50 = 8 nM Bind
Displacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation countingDisplacement of [125I]-PYY from human NPYY1 receptor overexpressed in CHO cell membrane after 120 mins by scintillation counting
477 7 1 9 3.4 Cc1nc(SCc2cc(N3CCS(=O)(=O)CC3)cc(NCc3cccc(F)n3)n2)oc1C
CHEMBL187490 npy1r_human Human No 8.1 IC50 = 8 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
619 9 4 9 4.9 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(N/C(=N/CCNC2CCN(c3cccc(Cl)c3)CC2)NC#N)c1
CHEMBL360188 npy1r_human Human No 8.1 IC50 = 8 nM Bind
Inhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptorsInhibition of binding of [125I]PYY to membranes of SK-N-MC cells expressing the human Y1 receptors
595 9 4 8 5.1 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)C1c1cccc(NC(=O)NCCNC2CCN(c3cccc(Cl)c3)CC2)c1
CHEMBL508974 npy1r_human Human No 8.1 IC50 = 8.2 nM Bind
Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysisAntagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL417912 npy1r_human Human No 8.1 IC50 = 8.4 nM Bind
Binding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYYBinding affinity against human recombinant NPY Y1 receptor in CHO/dhFr- cell membranes using [125I]PYY
560 13 2 8 6.8 CCc1sc(CCc2cc(OC(C)COC)cc(NCc3cc(Cl)cc(NC(=O)OC(C)C)c3)n2)nc1C
CHEMBL332347 npy1r_human Human Yes 8.1 IC50 = 8.8 nM Bind
Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL2314835 npy1r_human Human No 7.1 IC50 = 80 nM Bind
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)[C@H](CCCCNC(=O)COCC(=O)NCCOCCOCC(=O)NCC(=O)Nc1ccc(C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)cc1)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O
CHEMBL17441 npy1r_human Human No 5.1 IC50 = 8000 nM Bind
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
307 6 3 5 3.0 NCCCCNc1nc(N)c2cc(-c3ccccc3)ccc2n1
CHEMBL41457 npy1r_human Human No 7.1 IC50 = 81 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1
CHEMBL38531 npy1r_human Human No 5.1 IC50 = 8100 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
516 12 7 5 1.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccc(O)cc1
CHEMBL4759334 npy1r_human Human No 7.1 IC50 = 82 nM Funct
Agonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assayAgonist activity at human NPY1R expressed in HEK293 cells assessed as inhibition of adenosine-induced stimulation of cAMP accumulation by FRET assay
5831 196 92 80 -23.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)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)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL3214137 npy1r_human Human Yes 5.1 IC50 = 8303 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
386 6 1 3 5.0 O=C(CSCc1ccc(Cl)cc1)N/N=C/c1c(Cl)cccc1Cl
CHEMBL400631 npy1r_human Human No 6.1 IC50 = 832 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
564 7 2 6 4.9 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCN(CCO)CC1
CHEMBL1483730 npy1r_human Human Yes 5.1 IC50 = 8329 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
361 8 0 2 5.0 Cc1ccc(OCCCCN(C)Cc2ccccc2)c(Br)c1
CHEMBL1622175 npy1r_human Human Yes 5.1 IC50 = 8329 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
361 8 0 2 5.0 Cc1ccc(OCCCCN(C)Cc2ccccc2)c(Br)c1
CHEMBL1507807 npy1r_human Human Yes 5.1 IC50 = 8364 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
461 7 0 4 6.4 O=C(CCc1nc(-c2ccccc2)c(-c2ccccc2)o1)OCc1ccc(Br)cc1
CHEMBL17645 npy1r_human Human No 5.1 IC50 = 8370 nM Bind
Compound was tested for human Neuropeptide Y receptor type 1Compound was tested for human Neuropeptide Y receptor type 1
475 7 3 6 4.6 Nc1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12
CHEMBL163470 npy1r_human Human No 5.1 IC50 = 8500 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
525 8 2 4 5.0 O=S(=O)(NCCN1CCC(CNC2CCCc3ccc(Cl)cc3C2)CC1)c1cccc2ccccc12
CHEMBL1563162 npy1r_human Human Yes 5.1 IC50 = 8583 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
481 8 1 7 4.1 O=C(CN(Cc1ccc2c(c1)OCO2)C(=O)CSc1nc2ccccc2o1)NC1CCCCC1
CHEMBL238733 npy1r_human Human No 6.1 IC50 = 871 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
560 6 1 5 6.1 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@H]1F)N1CCN(C2CC2)CC1
CHEMBL528708 npy1r_human Human Yes 5.1 IC50 = 8751 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
258 5 1 2 3.5 CCCCCCn1c2c(c(=N)c3c1CCC3)CCC2
CHEMBL530291 npy1r_human Human Yes 5.1 IC50 = 8751 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
258 5 1 2 3.5 CCCCCCn1c2c(c(=N)c3c1CCC3)CCC2
CHEMBL1525599 npy1r_human Human Yes 5.1 IC50 = 8772 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
353 3 0 2 4.5 COc1ccccc1-n1c(-c2ccccc2)c[n+]2c1CCc1ccccc1-2
CHEMBL1623694 npy1r_human Human Yes 5.1 IC50 = 8772 nM Funct
PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]PUBCHEM_BIOASSAY: Dose response cell-based screening assay for antagonists of neuropeptide Y receptor Y1 (NPY-Y1). (Class of assay: confirmatory) [Related pubchem assays: 1040, 1255, 1254 ]
353 3 0 2 4.5 COc1ccccc1-n1c(-c2ccccc2)c[n+]2c1CCc1ccccc1-2
CHEMBL429698 npy1r_human Human No 7.1 IC50 = 88.3 nM Bind
Affinity against Neuropeptide Y receptor Y1 in SK-N-MC cell lineAffinity against Neuropeptide Y receptor Y1 in SK-N-MC cell line
None None None CC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C
CHEMBL1509886 npy1r_human Human Yes 5.1 IC50 = 8843 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
348 2 1 2 5.2 Cc1nc2ccc(F)cc2cc1C(=O)Nc1ccc(Cl)c(Cl)c1
CHEMBL17456 npy1r_human Human No 5.1 IC50 = 8900 nM Bind
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1Compound was tested for its affinity to bind with Neuropeptide Y receptor type 1
481 5 1 8 3.5 COc1cc2nc(N3CCC(N4C(=O)CC(C5CCCCC5)CC4=O)CC3)nc(N)c2cc1OC
CHEMBL3197426 npy1r_human Human Yes 5.1 IC50 = 8902 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
378 7 1 6 3.8 CCOc1ccc(Oc2c(/C=N/NC(C)=O)c(C)nn2-c2ccccc2)cc1
CHEMBL2397295 npy1r_human Human No 6.1 IC50 = 892 nM Bind
Displacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysisDisplacement of [125I]PYY from NPY1 receptor in human SK-N-MC cells after 1 hr by microbeta scintillation counting analysis
377 5 0 4 4.2 CCOc1cccc(C2(N3CCN(c4cccnc4)CC3)C3CC(C)CC32)c1
CHEMBL2314836 npy1r_human Human No 8.0 IC50 = 9.8 nM Bind
Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBNDisplacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN
None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)CC1)C(=O)O
CHEMBL41981 npy1r_human Human No 6.1 IC50 = 900 nM Funct
NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1
CHEMBL559593 npy1r_human Human No 5.1 IC50 = 9000 nM Funct
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation countingDisplacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
358 8 1 6 3.4 CCCNc1cc(N2CCOCC2)cc(CCc2nc(C)c(CC)o2)n1
CHEMBL1387309 npy1r_human Human Yes 5.1 IC50 = 9004 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
328 4 1 4 4.7 O=C(Nc1ccccc1)OCc1cc(-c2ccccc2Cl)on1
CHEMBL1377743 npy1r_human Human Yes 5.0 IC50 = 9045 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
338 6 0 6 4.0 Clc1ccc(OCCSc2nnnn2C2CCCCC2)cc1
CHEMBL1585652 npy1r_human Human Yes 5.0 IC50 = 9050 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
377 10 1 4 4.6 COc1ccccc1CCNCc1ccc(OC)c(OCc2ccccc2)c1
CHEMBL205261 npy1r_human Human No 7.0 IC50 = 93.3 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
534 6 1 6 5.4 CNC1CCC(Cn2c3c(c4ccccc42)C(=O)C(N2CCN(C)CC2)C[C@H]3Oc2ccc(Cl)cc2)CC1
CHEMBL1360426 npy1r_human Human Yes 5.0 IC50 = 9350 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
405 4 0 8 3.2 COc1ccc(-c2nnc3sc(C(C)N4C(=O)c5ccccc5C4=O)nn23)cc1
CHEMBL265766 npy1r_human Human No 6.0 IC50 = 945 nM Bind
Inhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cellsInhibition of I-PYY binding to Nueopeptide Y1 receptor expressed in human neuroblastoma SK-N-MC cells
607 10 3 9 5.7 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC)N1c1cccc(N/C(S)=N/CCCN2CCC(c3cccc(OC)c3)CC2)c1
CHEMBL1453832 npy1r_human Human Yes 5.0 IC50 = 9458 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
339 9 0 3 4.9 c1ccc(COc2ccc(OCCCCN3CCCCC3)cc2)cc1
CHEMBL1620870 npy1r_human Human Yes 5.0 IC50 = 9458 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
339 9 0 3 4.9 c1ccc(COc2ccc(OCCCCN3CCCCC3)cc2)cc1
CHEMBL238728 npy1r_human Human No 7.0 IC50 = 95 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
548 5 0 5 5.9 CN1CCN(C(=O)c2cc(Oc3ccc(Cl)cc3)c3c(c2)c2ccccc2n3C[C@@H]2CCN(C)C[C@H]2F)CC1
CHEMBL4765023 npy1r_human Human No 7.0 IC50 = 95.5 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
677 16 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)Cc1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803242 npy1r_human Human No 7.0 IC50 = 95.5 nM Funct
Antagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assayAntagonist activity at Y1 receptor in human HEL cells assessed as reduction in pNPY-induced calcium mobilization preincubated for 15 mins followed by pNPY stimulation and measured immediately by Fura-2 dye based fluorescence assay
677 16 7 5 3.1 N/C(=N/C(=O)NCCNC(=O)Cc1ccccc1)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL350620 npy1r_human Human No 5.0 IC50 = 9500 nM Bind
Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1Compound was evaluated for the inhibitory activity against human Neuropeptide Y receptor type 1
535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL350620 npy1r_human Human No 5.0 IC50 = 9600 nM Bind
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y1 receptor
535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2
CHEMBL204050 npy1r_human Human No 7.0 IC50 = 97.7 nM Bind
Displacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cellsDisplacement of [125I]PYY from human recombinant NPY1 receptor expressed in CHO cells
505 5 1 5 6.1 CC1CCN([C@@H]2C[C@@H](Oc3ccc(Cl)cc3)c3c(c4ccccc4n3CC3CCNCC3)C2=O)CC1
CHEMBL239774 npy1r_human Human No 5.0 IC50 = 9772 nM Bind
Displacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cellsDisplacement of [125]peptide YY from human recombinant Y1 receptor expressed in CHO cells
602 6 1 5 6.5 O=C(c1cc(Oc2ccc(Cl)cc2)c2c(c1)c1ccccc1n2C[C@@H]1CCNC[C@@H]1F)N1CCN(CC(F)(F)F)CC1
CHEMBL1527817 npy1r_human Human Yes 5.0 IC50 = 9798 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
390 2 1 6 3.8 Clc1ccc(C2=Nn3c(nnc3-c3[nH]nc4c3CCC4)SC2)cc1Cl
CHEMBL1603366 npy1r_human Human Yes 5.0 IC50 = 9957 nM Funct
PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]PUBCHEM_BIOASSAY: Dose response counterscreen for neuropeptide Y receptor Y2 (NPY-Y2): Cell-based high throughput assay to measure NPY-Y1 antagonism. (Class of assay: confirmatory) [Related pubchem assays: 1256, 793, 1257 ]
314 3 2 3 3.9 Cc1ccc(NC(S)=NCc2ccc3c(c2)OCO3)cc1C
CHEMBL3746386 npy1r_human Human No 10.6 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constantBinding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constant
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.6 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constantBinding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constant
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.6 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constantBinding affinity to NPY1R in human SK-N-MC cells assessed as kinetically derived dissociation rate constant
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 10.4 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cellsBinding affinity to NPY1R in human SK-N-MC cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.4 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cellsBinding affinity to NPY1R in human SK-N-MC cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.4 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cellsBinding affinity to NPY1R in human SK-N-MC cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 10.4 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells after 90 minsBinding affinity to NPY1R in human SK-N-MC cells after 90 mins
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.4 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells after 90 minsBinding affinity to NPY1R in human SK-N-MC cells after 90 mins
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.4 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells after 90 minsBinding affinity to NPY1R in human SK-N-MC cells after 90 mins
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 10.3 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysisBinding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.3 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysisBinding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.3 Kd = 0.0 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysisBinding affinity to NPY1R in human SK-N-MC cells by Scatchard plot analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 10.1 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7 cellsBinding affinity to NPY1R in human MCF7 cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.1 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7 cellsBinding affinity to NPY1R in human MCF7 cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.1 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7 cellsBinding affinity to NPY1R in human MCF7 cells
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 10.1 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysisBinding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 10.1 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysisBinding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 10.1 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysisBinding affinity to NPY1R in human MCF7-Y1 cells by Scatchard plot analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3746386 npy1r_human Human No 9.9 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysisBinding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747715 npy1r_human Human No 9.9 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysisBinding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL3747822 npy1r_human Human No 9.9 Kd = 0.1 nM Bind
Binding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysisBinding affinity to NPY1R in human MCF7 cells after 90 mins by microbeta2 plate counting analysis
615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL446342 npy1r_human Human No 9.0 Kd = 1.1 nM Bind
Binding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experiment
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL470495 npy1r_human Human No 9.0 Kd = 1.1 nM Bind
Binding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human MCF7 cells by kinetic experiment
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL446342 npy1r_human Human No 9.0 Kd = 1.1 nM Bind
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experiment
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL470495 npy1r_human Human No 9.0 Kd = 1.1 nM Bind
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experimentBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells by kinetic experiment
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL446342 npy1r_human Human No 8.9 Kd = 1.2 nM Bind
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cellsBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL470495 npy1r_human Human No 8.9 Kd = 1.2 nM Bind
Binding affinity to neuropeptide Y1 receptor in human SK-N-MC cellsBinding affinity to neuropeptide Y1 receptor in human SK-N-MC cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL446342 npy1r_human Human No 8.9 Kd = 1.2 nM Bind
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL470495 npy1r_human Human No 8.9 Kd = 1.2 nM Bind
Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cellsDisplacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL415353 npy1r_human Human No 7.0 Kd = 100 nM Bind
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
3395 75 48 47 -15.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@]1(C)NC(=O)CC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O
CHEMBL3559527 npy1r_human Human No 7.0 Kd = 100 nM Bind
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC
CHEMBL3746028 npy1r_human Human No 8.7 Kd = 2 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells by liquid scintillation counting assay
643 17 7 5 3.0 CCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL332347 npy1r_human Human Yes 8.7 Kd = 2.1 nM Bind
Binding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assayBinding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assay
473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O
CHEMBL446342 npy1r_human Human No 8.5 Kd = 2.9 nM Bind
Binding affinity to neuropeptide Y1 receptor in human MCF7 cellsBinding affinity to neuropeptide Y1 receptor in human MCF7 cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL470495 npy1r_human Human No 8.5 Kd = 2.9 nM Bind
Binding affinity to neuropeptide Y1 receptor in human MCF7 cellsBinding affinity to neuropeptide Y1 receptor in human MCF7 cells
529 12 5 4 2.9 CCC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL59832 npy1r_human Human Yes 4.4 Kd = 37153.5 nM Funct
pA2 for inhibition of NPY-stimulated [Ca2+] mobilization in HEL cellspA2 for inhibition of NPY-stimulated [Ca2+] mobilization in HEL cells
398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1
CHEMBL1774344 npy1r_human Human No 8.3 Kd = 5 nM Bind
Binding affinity at Y1R in human MCF-7 cells by flow cytometryBinding affinity at Y1R in human MCF-7 cells by flow cytometry
962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1
CHEMBL1789732 npy1r_human Human No 8.3 Kd = 5 nM Bind
Binding affinity at Y1R in human MCF-7 cells by flow cytometryBinding affinity at Y1R in human MCF-7 cells by flow cytometry
962 24 7 7 7.4 CN(C)c1ccc(/C=C/C=C/c2sc3ccccc3[n+]2CCCC(=O)NCCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)cc1
CHEMBL409167 npy1r_human Human Yes 6.1 Kd = 780 nM Bind
Displacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cellsDisplacement of l25I-PYY from Neuropeptide Y receptor type 1 of human neuroblastoma SK-N-MC cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC
CHEMBL4746035 npy1r_human Human No 10.5 Ki = 0.0 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802520 npy1r_human Human No 10.5 Ki = 0.0 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
619 15 7 5 1.8 N/C(=N/C(=O)NCCNC(=O)CF)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assayDisplacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL349328 npy1r_human Human No 10.3 Ki = 0.1 nM Bind
Ability to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cellsAbility to displace [125I]-peptide YY binding to cloned human Neuropeptide Y receptor type 1 expressed in AV-12 cells
720 15 0 6 8.2 Ic1ccc(CCN2CCC(CCCn3c(COc4ccccc4)nc4c(OCCCN5CCCCC5)cccc43)CC2)cc1
CHEMBL4794692 npy1r_human Human No 10.3 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803933 npy1r_human Human No 10.3 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
635 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)CCl)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4743976 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
601 14 7 5 1.9 CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802480 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
601 14 7 5 1.9 CC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL508974 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)
602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL511460 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)Displacement of [3H]propionyl-pNPY from NPY1R (unknown origin)
544 12 6 4 2.7 CCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4762668 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
615 15 7 5 2.2 CC(=O)NCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4803176 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
615 15 7 5 2.2 CC(=O)NCCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4743858 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL4802419 npy1r_human Human No 10.2 Ki = 0.1 nM Bind
Displacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assayDisplacement of [3H]UR-MK299 from Y1 receptor in human SK-N-MC cells by radioligand binding assay
637 15 7 5 2.1 N/C(=N/C(=O)NCCNC(=O)C(F)F)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1
CHEMBL2110365 npy1r_human Human Yes 10.2 Ki = 0.1 nM Bind