Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
|
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
CHEMBL2165920 | 211792 | None | 25 | Human | Functional | pEC50 | = | 8.8 | 8.8 | 21 | 2 | Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm300535s | ||||
44542324 | 200456 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 242 | 3 | 3 | 3 | 2.1 | Cc1ccccc1-c1ccc(/C=N/NC(=N)N)o1 | 10.1021/jm9011998 | ||
CHEMBL573738 | 200456 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 242 | 3 | 3 | 3 | 2.1 | Cc1ccccc1-c1ccc(/C=N/NC(=N)N)o1 | 10.1021/jm9011998 | ||
44542328 | 200573 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -2 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 296 | 3 | 3 | 3 | 2.8 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 | 10.1021/jm9011998 | ||
CHEMBL4785076 | 200573 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -2 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 296 | 3 | 3 | 3 | 2.8 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 | 10.1021/jm9011998 | ||
CHEMBL574565 | 200573 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -2 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 296 | 3 | 3 | 3 | 2.8 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 | 10.1021/jm9011998 | ||
9573348 | 200313 | None | 4 | Human | Functional | pEC50 | = | 6 | 6.0 | 14 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 230 | 2 | 3 | 2 | 1.8 | N=C(N)N/N=C/c1ccc(Cl)c(Cl)c1 | 10.1021/jm9011998 | ||
CHEMBL3982697 | 200313 | None | 4 | Human | Functional | pEC50 | = | 6 | 6.0 | 14 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 230 | 2 | 3 | 2 | 1.8 | N=C(N)N/N=C/c1ccc(Cl)c(Cl)c1 | 10.1021/jm9011998 | ||
CHEMBL572531 | 200313 | None | 4 | Human | Functional | pEC50 | = | 6 | 6.0 | 14 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 230 | 2 | 3 | 2 | 1.8 | N=C(N)N/N=C/c1ccc(Cl)c(Cl)c1 | 10.1021/jm9011998 | ||
172439679 | 195348 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -44 | 4 | Agonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay |
ChEMBL | 1150 | 24 | 13 | 13 | -0.4 | CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.3c02093 | ||
CHEMBL5401796 | 195348 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -44 | 4 | Agonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay |
ChEMBL | 1150 | 24 | 13 | 13 | -0.4 | CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.3c02093 | ||
CHEMBL5086601 | 217528 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -3 | 5 | Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay |
ChEMBL | None | None | None | CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.1c00694 | ||||
CHEMBL5086601 | 217528 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -3 | 5 | Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay |
ChEMBL | None | None | None | CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.1c00694 | ||||
1485 | 631 | None | 27 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -20 | 2 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 473 | 11 | 5 | 4 | 2.4 | O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O | 10.1021/jm300535s | ||
3474 | 631 | None | 27 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -20 | 2 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 473 | 11 | 5 | 4 | 2.4 | O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O | 10.1021/jm300535s | ||
5311023 | 631 | None | 27 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -20 | 2 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 473 | 11 | 5 | 4 | 2.4 | O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O | 10.1021/jm300535s | ||
CHEMBL332347 | 631 | None | 27 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -20 | 2 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 473 | 11 | 5 | 4 | 2.4 | O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O | 10.1021/jm300535s | ||
44542178 | 201217 | None | 6 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 264 | 2 | 3 | 2 | 2.2 | N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 | 10.1021/jm300535s | ||
CHEMBL4794542 | 201217 | None | 6 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 264 | 2 | 3 | 2 | 2.2 | N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 | 10.1021/jm300535s | ||
CHEMBL583068 | 201217 | None | 6 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 264 | 2 | 3 | 2 | 2.2 | N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 | 10.1021/jm300535s | ||
123797 | 2791 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 4 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm300535s | ||||
1479 | 2791 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 4 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm300535s | ||||
CHEMBL429731 | 2791 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 4 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm300535s | ||||
162648597 | 179865 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 5 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1116 | 23 | 14 | 15 | -2.8 | N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.0c01367 | ||
CHEMBL4744365 | 179865 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 5 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1116 | 23 | 14 | 15 | -2.8 | N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.0c01367 | ||
162648597 | 179865 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 5 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1116 | 23 | 14 | 15 | -2.8 | N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.0c01367 | ||
CHEMBL4744365 | 179865 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 5 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1116 | 23 | 14 | 15 | -2.8 | N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.0c01367 | ||
44542332 | 200429 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 309 | 3 | 3 | 3 | 2.5 | Cn1c(/C=N/NC(=N)N)ccc1-c1ccccc1C(F)(F)F | 10.1021/jm9011998 | ||
CHEMBL573519 | 200429 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 309 | 3 | 3 | 3 | 2.5 | Cn1c(/C=N/NC(=N)N)ccc1-c1ccccc1C(F)(F)F | 10.1021/jm9011998 | ||
60168134 | 82140 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 2 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 374 | 3 | 3 | 3 | 3.5 | N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1 | 10.1021/jm300535s | ||
CHEMBL2165921 | 82140 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 2 | Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | 374 | 3 | 3 | 3 | 3.5 | N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1 | 10.1021/jm300535s | ||
44542176 | 200404 | None | 7 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 1 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 318 | 2 | 3 | 2 | 2.0 | N=C(N)N/N=C/c1ccc(Br)c(Br)c1 | 10.1021/jm9011998 | ||
CHEMBL4784123 | 200404 | None | 7 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 1 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 318 | 2 | 3 | 2 | 2.0 | N=C(N)N/N=C/c1ccc(Br)c(Br)c1 | 10.1021/jm9011998 | ||
CHEMBL573297 | 200404 | None | 7 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 1 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 318 | 2 | 3 | 2 | 2.0 | N=C(N)N/N=C/c1ccc(Br)c(Br)c1 | 10.1021/jm9011998 | ||
123797 | 2791 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 4 | Agonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm300535s | ||||
1479 | 2791 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 4 | Agonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm300535s | ||||
CHEMBL429731 | 2791 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 4 | Agonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm300535s | ||||
CHEMBL5094675 | 217999 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 5 | Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay |
ChEMBL | None | None | None | CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.1c00694 | ||||
162654268 | 180781 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 4 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1126 | 33 | 15 | 14 | -3.7 | CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.6b01181 | ||
CHEMBL4755334 | 180781 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 4 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1126 | 33 | 15 | 14 | -3.7 | CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.6b01181 | ||
162654268 | 180781 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 4 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1126 | 33 | 15 | 14 | -3.7 | CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.6b01181 | ||
CHEMBL4755334 | 180781 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 4 | Agonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR2 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay |
ChEMBL | 1126 | 33 | 15 | 14 | -3.7 | CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.6b01181 | ||
CHEMBL5094675 | 217999 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 5 | Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay |
ChEMBL | None | None | None | CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.1c00694 | ||||
172466389 | 196630 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -51 | 4 | Agonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay |
ChEMBL | 1136 | 24 | 13 | 13 | -0.8 | CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.3c02093 | ||
CHEMBL5428360 | 196630 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -51 | 4 | Agonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay |
ChEMBL | 1136 | 24 | 13 | 13 | -0.8 | CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 | 10.1021/acs.jmedchem.3c02093 | ||
162662402 | 182036 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 5 hrs by firefly/renilla luciferase reporter assayAgonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 5 hrs by firefly/renilla luciferase reporter assay |
ChEMBL | 520 | 6 | 1 | 7 | 5.6 | COc1cc2c(c(OC)c1OC)-c1c(cc(C)c(C)c1OC)[C@@H](C(=O)Oc1ccccc1)[C@@](C)(O)[C@@H](C)C2 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4779743 | 182036 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 5 hrs by firefly/renilla luciferase reporter assayAgonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 5 hrs by firefly/renilla luciferase reporter assay |
ChEMBL | 520 | 6 | 1 | 7 | 5.6 | COc1cc2c(c(OC)c1OC)-c1c(cc(C)c(C)c1OC)[C@@H](C(=O)Oc1ccccc1)[C@@](C)(O)[C@@H](C)C2 | 10.1021/acs.jmedchem.0c00643 | ||
155520785 | 170612 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 2 | 4 | Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins |
ChEMBL | 1165 | 30 | 12 | 11 | 2.7 | N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O | 10.1016/j.bmc.2019.01.003 | ||
CHEMBL4449491 | 170612 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 2 | 4 | Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins |
ChEMBL | 1165 | 30 | 12 | 11 | 2.7 | N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O | 10.1016/j.bmc.2019.01.003 | ||
44542330 | 200428 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | Agonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF2 receptor expressed in cells assessed as beta-galactosidase levels after 5 days |
ChEMBL | 312 | 3 | 3 | 3 | 3.3 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)s1 | 10.1021/jm9011998 |
Showing 1 to 50 of 252 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
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Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
44542328 | 200573 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 296 | 3 | 3 | 3 | 2.8 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4785076 | 200573 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 296 | 3 | 3 | 3 | 2.8 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL574565 | 200573 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 296 | 3 | 3 | 3 | 2.8 | N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 | 10.1021/acs.jmedchem.0c00643 | ||
162676940 | 183434 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assay |
ChEMBL | 897 | 23 | 13 | 10 | -1.0 | Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4797394 | 183434 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assay |
ChEMBL | 897 | 23 | 13 | 10 | -1.0 | Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O | 10.1021/acs.jmedchem.0c00643 | ||
155461914 | 182927 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assay |
ChEMBL | 1014 | 25 | 10 | 10 | 2.5 | Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4790994 | 182927 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR2 expressed in CHO cells by [35S]-GTP S binding assay |
ChEMBL | 1014 | 25 | 10 | 10 | 2.5 | Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL3360830 | 214035 | None | 0 | Human | Binding | pEC50 | = | 8.6 | 8.6 | 6 | 2 | Agonist activity at human NPFF2 receptorAgonist activity at human NPFF2 receptor |
ChEMBL | None | None | None | CC(C)C[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](N)Cc1ccc(O)cc1 | 10.1021/jm500989n | ||||
9942758 | 183594 | None | 0 | Rat | Binding | pEC50 | = | 6.4 | 6.4 | -11 | 4 | Agonist activity at rat NPFFR2Agonist activity at rat NPFFR2 |
ChEMBL | 234 | 1 | 3 | 2 | 2.5 | Cc1cc(NC(=N)N)nc2ccc(Cl)cc12 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4799458 | 183594 | None | 0 | Rat | Binding | pEC50 | = | 6.4 | 6.4 | -11 | 4 | Agonist activity at rat NPFFR2Agonist activity at rat NPFFR2 |
ChEMBL | 234 | 1 | 3 | 2 | 2.5 | Cc1cc(NC(=N)N)nc2ccc(Cl)cc12 | 10.1021/acs.jmedchem.0c00643 | ||
44542178 | 201217 | None | 6 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 264 | 2 | 3 | 2 | 2.2 | N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4794542 | 201217 | None | 6 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 264 | 2 | 3 | 2 | 2.2 | N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL583068 | 201217 | None | 6 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 264 | 2 | 3 | 2 | 2.2 | N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 | 10.1021/acs.jmedchem.0c00643 | ||
9573348 | 200313 | None | 4 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 230 | 2 | 3 | 2 | 1.8 | N=C(N)N/N=C/c1ccc(Cl)c(Cl)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL3982697 | 200313 | None | 4 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 230 | 2 | 3 | 2 | 1.8 | N=C(N)N/N=C/c1ccc(Cl)c(Cl)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL572531 | 200313 | None | 4 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 230 | 2 | 3 | 2 | 1.8 | N=C(N)N/N=C/c1ccc(Cl)c(Cl)c1 | 10.1021/acs.jmedchem.0c00643 | ||
44542176 | 200404 | None | 7 | Human | Binding | pEC50 | = | 6.1 | 6.1 | -1 | 2 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 318 | 2 | 3 | 2 | 2.0 | N=C(N)N/N=C/c1ccc(Br)c(Br)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4784123 | 200404 | None | 7 | Human | Binding | pEC50 | = | 6.1 | 6.1 | -1 | 2 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 318 | 2 | 3 | 2 | 2.0 | N=C(N)N/N=C/c1ccc(Br)c(Br)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL573297 | 200404 | None | 7 | Human | Binding | pEC50 | = | 6.1 | 6.1 | -1 | 2 | Agonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR2 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay |
ChEMBL | 318 | 2 | 3 | 2 | 2.0 | N=C(N)N/N=C/c1ccc(Br)c(Br)c1 | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL1672379 | 211289 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | None | None | None | None | 10.1021/ml1002053 | ||||
16735569 | 142421 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | 798 | 21 | 10 | 7 | 1.3 | CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O | 10.1021/ml1002053 | ||
CHEMBL388586 | 142421 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | 798 | 21 | 10 | 7 | 1.3 | CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O | 10.1021/ml1002053 | ||
25138123 | 179353 | None | 0 | Human | Binding | pIC50 | = | 5.6 | 5.6 | - | 0 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | 781 | 21 | 9 | 6 | 2.9 | CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O | 10.1021/ml1002053 | ||
CHEMBL472833 | 179353 | None | 0 | Human | Binding | pIC50 | = | 5.6 | 5.6 | - | 0 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | 781 | 21 | 9 | 6 | 2.9 | CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O | 10.1021/ml1002053 | ||
1281 | 2187 | None | 32 | Human | Binding | pIC50 | = | 7.1 | 7.1 | - | 2 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | None | None | None | None | 10.1021/ml1002053 | ||||
1283 | 2187 | None | 32 | Human | Binding | pIC50 | = | 7.1 | 7.1 | - | 2 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | None | None | None | None | 10.1021/ml1002053 | ||||
25240297 | 2187 | None | 32 | Human | Binding | pIC50 | = | 7.1 | 7.1 | - | 2 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | None | None | None | None | 10.1021/ml1002053 | ||||
CHEMBL376756 | 2187 | None | 32 | Human | Binding | pIC50 | = | 7.1 | 7.1 | - | 2 | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs |
ChEMBL | None | None | None | None | 10.1021/ml1002053 | ||||
123797 | 2791 | None | 21 | Human | Binding | pKd | = | 9.7 | 9.7 | 1 | 4 | Binding affinity to human NPFFR2Binding affinity to human NPFFR2 |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.0c00643 | ||||
1479 | 2791 | None | 21 | Human | Binding | pKd | = | 9.7 | 9.7 | 1 | 4 | Binding affinity to human NPFFR2Binding affinity to human NPFFR2 |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.0c00643 | ||||
CHEMBL429731 | 2791 | None | 21 | Human | Binding | pKd | = | 9.7 | 9.7 | 1 | 4 | Binding affinity to human NPFFR2Binding affinity to human NPFFR2 |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.0c00643 | ||||
123797 | 2791 | None | 21 | Human | Binding | pKd | = | 9.4 | 9.4 | 1 | 4 | Binding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assayBinding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.0c00643 | ||||
1479 | 2791 | None | 21 | Human | Binding | pKd | = | 9.4 | 9.4 | 1 | 4 | Binding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assayBinding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.0c00643 | ||||
CHEMBL429731 | 2791 | None | 21 | Human | Binding | pKd | = | 9.4 | 9.4 | 1 | 4 | Binding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assayBinding affinity to human NPFFR2 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.0c00643 | ||||
CHEMBL3786309 | 214723 | None | 0 | Human | Binding | pKd | = | 9.3 | 9.3 | - | 1 | Binding affinity to human NPFF2 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrophotometric countingBinding affinity to human NPFF2 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrophotometric counting |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.5b01495 | ||||
123797 | 2791 | None | 21 | Human | Binding | pKi | = | 10.7 | 10.7 | 1 | 4 | Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.1c00256 | ||||
1479 | 2791 | None | 21 | Human | Binding | pKi | = | 10.7 | 10.7 | 1 | 4 | Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.1c00256 | ||||
CHEMBL429731 | 2791 | None | 21 | Human | Binding | pKi | = | 10.7 | 10.7 | 1 | 4 | Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.1c00256 | ||||
102080626 | 171398 | None | 0 | Human | Binding | pKi | = | 10.6 | 10.6 | 107 | 2 | Displacement of [125I]EYF from human NPFFR2 expressed in CHO cells by gamma-counter methodDisplacement of [125I]EYF from human NPFFR2 expressed in CHO cells by gamma-counter method |
ChEMBL | 1377 | 39 | 15 | 16 | -3.5 | CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N(C)C(=O)[C@@H]1CCCN1C(=O)[C@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL4460742 | 171398 | None | 0 | Human | Binding | pKi | = | 10.6 | 10.6 | 107 | 2 | Displacement of [125I]EYF from human NPFFR2 expressed in CHO cells by gamma-counter methodDisplacement of [125I]EYF from human NPFFR2 expressed in CHO cells by gamma-counter method |
ChEMBL | 1377 | 39 | 15 | 16 | -3.5 | CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N(C)C(=O)[C@@H]1CCCN1C(=O)[C@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/acs.jmedchem.0c00643 | ||
CHEMBL414263 | 215578 | None | 4 | Rat | Binding | pKi | = | 9.8 | 9.8 | 2 | 4 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm00047a005 | ||||
CHEMBL385751 | 214825 | None | 0 | Rat | Binding | pKi | = | 9.7 | 9.7 | - | 1 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | CC(C)C[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm00047a005 | ||||
CHEMBL269186 | 213240 | None | 9 | Rat | Binding | pKi | = | 9.7 | 9.7 | - | 1 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm00047a005 | ||||
CHEMBL420318 | 215704 | None | 0 | Rat | Binding | pKi | = | 9.7 | 9.7 | - | 1 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm00047a005 | ||||
123797 | 2791 | None | 21 | Rat | Binding | pKi | = | 9.7 | 9.7 | -1 | 4 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | None | 10.1021/jm00047a005 | ||||
1479 | 2791 | None | 21 | Rat | Binding | pKi | = | 9.7 | 9.7 | -1 | 4 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | None | 10.1021/jm00047a005 | ||||
CHEMBL429731 | 2791 | None | 21 | Rat | Binding | pKi | = | 9.7 | 9.7 | -1 | 4 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | None | 10.1021/jm00047a005 | ||||
CHEMBL386065 | 214834 | None | 0 | Rat | Binding | pKi | = | 9.7 | 9.7 | - | 1 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm00047a005 | ||||
CHEMBL331606 | 213840 | None | 0 | Rat | Binding | pKi | = | 9.4 | 9.4 | - | 1 | Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFFBinding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF |
ChEMBL | None | None | None | NC(=O)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | 10.1021/jm00047a005 | ||||
CHEMBL3360830 | 214035 | None | 0 | Human | Binding | pKi | = | 9.3 | 9.3 | 6 | 2 | Displacement of [3H]EYF from human NPFF2 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]EYF from human NPFF2 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis |
ChEMBL | None | None | None | CC(C)C[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](N)Cc1ccc(O)cc1 | 10.1021/jm500989n |
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