Ligand source activities (1 row/activity)
| 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
| |
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
| |
| CHEMBL342252 | 214132 | None | 0 | Rat | Functional | pEC50 | = | 11 | 11.0 | 2 | 4 | Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay |
ChEMBL | None | None | None | CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/jm5003843 | ||||
| 1574 | 2809 | None | 18 | Rat | Functional | pEC50 | = | 10.4 | 10.4 | 26 | 6 | Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1021/jm5003843 | ||||
| 1579 | 2809 | None | 18 | Rat | Functional | pEC50 | = | 10.4 | 10.4 | 26 | 6 | Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1021/jm5003843 | ||||
| 25077406 | 2809 | None | 18 | Rat | Functional | pEC50 | = | 10.4 | 10.4 | 26 | 6 | Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1021/jm5003843 | ||||
| 3830 | 2809 | None | 18 | Rat | Functional | pEC50 | = | 10.4 | 10.4 | 26 | 6 | Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1021/jm5003843 | ||||
| CHEMBL407196 | 2809 | None | 18 | Rat | Functional | pEC50 | = | 10.4 | 10.4 | 26 | 6 | Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1021/jm5003843 | ||||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 2 | 3 | Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assayAgonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2014.06.033 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 2 | 3 | Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assayAgonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2014.06.033 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 2 | 3 | Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assayAgonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2014.06.033 | ||||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 2 | 3 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00462 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 2 | 3 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00462 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 2 | 3 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00462 | ||||
| 1574 | 2809 | None | 18 | Human | Functional | pEC50 | = | 9.6 | 9.6 | -26 | 6 | Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assayAgonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.01.024 | ||||
| 1579 | 2809 | None | 18 | Human | Functional | pEC50 | = | 9.6 | 9.6 | -26 | 6 | Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assayAgonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.01.024 | ||||
| 25077406 | 2809 | None | 18 | Human | Functional | pEC50 | = | 9.6 | 9.6 | -26 | 6 | Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assayAgonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.01.024 | ||||
| 3830 | 2809 | None | 18 | Human | Functional | pEC50 | = | 9.6 | 9.6 | -26 | 6 | Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assayAgonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.01.024 | ||||
| CHEMBL407196 | 2809 | None | 18 | Human | Functional | pEC50 | = | 9.6 | 9.6 | -26 | 6 | Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assayAgonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.01.024 | ||||
| 155569717 | 176344 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | 1657 | 48 | 16 | 20 | 4.4 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)NC(=O)NCCOCCOCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
| CHEMBL4537266 | 176344 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | 1657 | 48 | 16 | 20 | 4.4 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)NC(=O)NCCOCCOCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
| CHEMBL4594723 | 176344 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | 1657 | 48 | 16 | 20 | 4.4 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)NC(=O)NCCOCCOCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 2 | 3 | Agonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assayAgonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 2 | 3 | Agonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assayAgonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 2 | 3 | Agonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assayAgonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 155569737 | 176740 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | 1597 | 44 | 16 | 18 | 5.1 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)NC(=O)NCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
| CHEMBL4457798 | 176740 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | 1597 | 44 | 16 | 18 | 5.1 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)NC(=O)NCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
| CHEMBL4597941 | 176740 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | - | 1 | Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assayAgonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay |
ChEMBL | 1597 | 44 | 16 | 18 | 5.1 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)NC(=O)NCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assayAgonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assayAgonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assayAgonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assayAgonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assayAgonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assayAgonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assayAgonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assayAgonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 2 | 3 | Agonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assayAgonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00175 | ||||
| 172460862 | 196280 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 818 | 24 | 11 | 11 | -2.0 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCON=C(N)N)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL5420374 | 196280 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 818 | 24 | 11 | 11 | -2.0 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCON=C(N)N)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL504768 | 216672 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assayAgonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assay |
ChEMBL | None | None | None | CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)N=[N+]=[N-])C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/jm801072v | ||||
| 168475922 | 197197 | None | 2 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 790 | 24 | 10 | 11 | -0.9 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCON=C(N)N)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL5441066 | 197197 | None | 2 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 790 | 24 | 10 | 11 | -0.9 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCON=C(N)N)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| 172440132 | 195368 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 790 | 24 | 10 | 11 | -0.9 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCON=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL5402152 | 195368 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 790 | 24 | 10 | 11 | -0.9 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCON=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL468951 | 216511 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assayAgonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assay |
ChEMBL | None | None | None | CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/jm801072v | ||||
| 1569 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2 | 3 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2023.115386 | ||||
| 5311318 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2 | 3 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2023.115386 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 2 | 3 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2023.115386 | ||||
| 172468416 | 196926 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 818 | 24 | 11 | 11 | -2.0 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)CCON=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL5434985 | 196926 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assayAgonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay |
ChEMBL | 818 | 24 | 11 | 11 | -2.0 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)CCON=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1016/j.ejmech.2023.115386 | ||
| CHEMBL342252 | 214132 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | -2 | 4 | Agonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assayAgonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assay |
ChEMBL | None | None | None | CC[C@@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/jm801072v | ||||
| 127030965 | 139290 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | - | 1 | Agonist activity at human neurotensin receptor 1 in HT-29 cells assessed as intracellular calcium mobilization by Fura-2 dye based spectrofluorimetry analysisAgonist activity at human neurotensin receptor 1 in HT-29 cells assessed as intracellular calcium mobilization by Fura-2 dye based spectrofluorimetry analysis |
ChEMBL | 1396 | 38 | 14 | 12 | 6.0 | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCN/C(N)=N/C(=O)NCCCCNC(=O)CCCCCN1/C(=C\C=C\C=C\C2=[N+](C)c3ccccc3C2(C)C)C(C)(C)c2ccccc21)C(=O)N[C@@H](CC(C)C)C(=O)O | 10.1021/acsmedchemlett.9b00462 | ||
Showing 1 to 50 of 706 entries
| 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
| |
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
| |
| 644241 | 95239 | None | 68 | Human | Binding | pAC50 | = | 5.0 | 5.0 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 529 | 6 | 2 | 7 | 6.4 | Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cccnc5)n4)c3)cc(C(F)(F)F)c2)cn1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL255863 | 95239 | None | 68 | Human | Binding | pAC50 | = | 5.0 | 5.0 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 529 | 6 | 2 | 7 | 6.4 | Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cccnc5)n4)c3)cc(C(F)(F)F)c2)cn1 | 10.1038/s41467-023-40064-9 | ||
| 2519 | 779 | None | 49 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 12 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 194 | 0 | 0 | 6 | -1.0 | Cn1cnc2c1c(=O)n(C)c(=O)n2C | 10.1038/s41467-023-40064-9 | ||
| 2519.0 | 779 | None | 49 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 12 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 194 | 0 | 0 | 6 | -1.0 | Cn1cnc2c1c(=O)n(C)c(=O)n2C | 10.1038/s41467-023-40064-9 | ||
| 407 | 779 | None | 49 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 12 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 194 | 0 | 0 | 6 | -1.0 | Cn1cnc2c1c(=O)n(C)c(=O)n2C | 10.1038/s41467-023-40064-9 | ||
| 463 | 779 | None | 49 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 12 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 194 | 0 | 0 | 6 | -1.0 | Cn1cnc2c1c(=O)n(C)c(=O)n2C | 10.1038/s41467-023-40064-9 | ||
| CHEMBL113 | 779 | None | 49 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 12 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 194 | 0 | 0 | 6 | -1.0 | Cn1cnc2c1c(=O)n(C)c(=O)n2C | 10.1038/s41467-023-40064-9 | ||
| DB00201 | 779 | None | 49 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 12 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 194 | 0 | 0 | 6 | -1.0 | Cn1cnc2c1c(=O)n(C)c(=O)n2C | 10.1038/s41467-023-40064-9 | ||
| 2997 | 193260 | None | 19 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 270 | 1 | 1 | 2 | 3.1 | O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL523 | 193260 | None | 19 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 270 | 1 | 1 | 2 | 3.1 | O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1 | 10.1038/s41467-023-40064-9 | ||
| 8730 | 198347 | None | 44 | Human | Binding | pAC50 | = | 5.3 | 5.3 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 777 | 5 | 3 | 4 | 4.6 | N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O | 10.1038/s41467-023-40064-9 | ||
| 90657408 | 198347 | None | 44 | Human | Binding | pAC50 | = | 5.3 | 5.3 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 777 | 5 | 3 | 4 | 4.6 | N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O | 10.1038/s41467-023-40064-9 | ||
| CHEMBL559 | 198347 | None | 44 | Human | Binding | pAC50 | = | 5.3 | 5.3 | - | 0 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 777 | 5 | 3 | 4 | 4.6 | N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O | 10.1038/s41467-023-40064-9 | ||
| 5411 | 206491 | None | 57 | Human | Binding | pAC50 | = | 5 | 5.0 | - | 2 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 264 | 8 | 1 | 4 | 2.6 | CCCCNc1ccc(C(=O)OCCN(C)C)cc1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL698 | 206491 | None | 57 | Human | Binding | pAC50 | = | 5 | 5.0 | - | 2 | Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 264 | 8 | 1 | 4 | 2.6 | CCCCNc1ccc(C(=O)OCCN(C)C)cc1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL3622803 | 214342 | None | 0 | Human | Binding | pEC50 | = | 9.5 | 9.5 | - | 0 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | C[Si](C)(C)C[C@H](NC(=O)[C@H](C[Si](C)(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCCN)C(=O)O | 10.1021/acs.jmedchem.5b00841 | ||||
| 1569 | 2126 | None | 31 | Rat | Binding | pEC50 | = | 8.9 | 8.9 | - | 2 | Agonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contractionAgonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contraction |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| 5311318 | 2126 | None | 31 | Rat | Binding | pEC50 | = | 8.9 | 8.9 | - | 2 | Agonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contractionAgonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contraction |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| CHEMBL415788 | 2126 | None | 31 | Rat | Binding | pEC50 | = | 8.9 | 8.9 | - | 2 | Agonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contractionAgonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contraction |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| CHEMBL3622802 | 214341 | None | 0 | Rat | Binding | pEC50 | = | 8.9 | 8.9 | - | 0 | Agonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contractionAgonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contraction |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C[Si](C)(C)C)C(=O)O | 10.1021/acs.jmedchem.5b00841 | ||||
| 1569 | 2126 | None | 31 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 2 | 2 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| 5311318 | 2126 | None | 31 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 2 | 2 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Binding | pEC50 | = | 8.9 | 8.9 | 2 | 2 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| CHEMBL3622802 | 214341 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C[Si](C)(C)C)C(=O)O | 10.1021/acs.jmedchem.5b00841 | ||||
| CHEMBL3622802 | 214341 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C[Si](C)(C)C)C(=O)O | 10.1021/acs.jmedchem.5b00841 | ||||
| 1569 | 2126 | None | 31 | Human | Binding | pEC50 | = | 8.7 | 8.7 | 2 | 2 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| 5311318 | 2126 | None | 31 | Human | Binding | pEC50 | = | 8.7 | 8.7 | 2 | 2 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| CHEMBL415788 | 2126 | None | 31 | Human | Binding | pEC50 | = | 8.7 | 8.7 | 2 | 2 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.5b00841 | ||||
| 16127648 | 14370 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 1 | Binding affinity to human NTR1 by gamma countingBinding affinity to human NTR1 by gamma counting |
ChEMBL | 817 | 22 | 9 | 8 | 1.4 | CC(C)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)CCC[N+](C)(C)C)C(C)(C)C)C(=O)O | 10.1021/jm100092s | ||
| CHEMBL1172376 | 14370 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 1 | Binding affinity to human NTR1 by gamma countingBinding affinity to human NTR1 by gamma counting |
ChEMBL | 817 | 22 | 9 | 8 | 1.4 | CC(C)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)CCC[N+](C)(C)C)C(C)(C)C)C(=O)O | 10.1021/jm100092s | ||
| CHEMBL1200171 | 14370 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 1 | Binding affinity to human NTR1 by gamma countingBinding affinity to human NTR1 by gamma counting |
ChEMBL | 817 | 22 | 9 | 8 | 1.4 | CC(C)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)CCC[N+](C)(C)C)C(C)(C)C)C(=O)O | 10.1021/jm100092s | ||
| 1580 | 3665 | None | 36 | Human | Binding | pEC50 | = | 5 | 5.0 | 1 | 4 | Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assayAgonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay |
ChEMBL | 685 | 13 | 2 | 8 | 5.7 | COc1cccc(c1c1cc(nn1c1ccc(cc1C(C)C)C(=O)N(CCCN(C)C)C)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC | 10.1021/ml400176n | ||
| 5311451 | 3665 | None | 36 | Human | Binding | pEC50 | = | 5 | 5.0 | 1 | 4 | Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assayAgonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay |
ChEMBL | 685 | 13 | 2 | 8 | 5.7 | COc1cccc(c1c1cc(nn1c1ccc(cc1C(C)C)C(=O)N(CCCN(C)C)C)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC | 10.1021/ml400176n | ||
| CHEMBL3040381 | 3665 | None | 36 | Human | Binding | pEC50 | = | 5 | 5.0 | 1 | 4 | Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assayAgonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay |
ChEMBL | 685 | 13 | 2 | 8 | 5.7 | COc1cccc(c1c1cc(nn1c1ccc(cc1C(C)C)C(=O)N(CCCN(C)C)C)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC | 10.1021/ml400176n | ||
| 53245521 | 92455 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assayAgonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay |
ChEMBL | 404 | 5 | 0 | 6 | 4.2 | COc1ccc2nc(C3CCC3)nc(N3CCN(c4ccccc4OC)CC3)c2c1 | 10.1021/ml400176n | ||
| CHEMBL2431125 | 92455 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assayAgonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay |
ChEMBL | 404 | 5 | 0 | 6 | 4.2 | COc1ccc2nc(C3CCC3)nc(N3CCN(c4ccccc4OC)CC3)c2c1 | 10.1021/ml400176n | ||
| 118610278 | 169613 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 430 | 7 | 0 | 5 | 5.7 | CCCN(C)c1ccc2c(N3CCC(c4ccccc4OC)CC3)nc(C3CC3)nc2c1 | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL4434705 | 169613 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 430 | 7 | 0 | 5 | 5.7 | CCCN(C)c1ccc2c(N3CCC(c4ccccc4OC)CC3)nc(C3CC3)nc2c1 | 10.1021/acs.jmedchem.9b00340 | ||
| 118617781 | 175291 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 444 | 5 | 1 | 6 | 4.5 | COc1ccccc1C1CCN(c2nc(C3CC3)nc3ccc(N4CC[C@H](O)C4)cc23)CC1 | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL4570744 | 175291 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 444 | 5 | 1 | 6 | 4.5 | COc1ccccc1C1CCN(c2nc(C3CC3)nc3ccc(N4CC[C@H](O)C4)cc23)CC1 | 10.1021/acs.jmedchem.9b00340 | ||
| 90237596 | 172252 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 419 | 6 | 0 | 6 | 4.9 | COc1cc2nc(C3CC3)nc(N3CCC(c4ccccc4OC)CC3)c2cc1OC | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL4473181 | 172252 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 419 | 6 | 0 | 6 | 4.9 | COc1cc2nc(C3CC3)nc(N3CCC(c4ccccc4OC)CC3)c2cc1OC | 10.1021/acs.jmedchem.9b00340 | ||
| 118610372 | 172063 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 446 | 7 | 1 | 6 | 4.7 | COc1ccccc1C1CCN(c2nc(C3CCC3)nc3ccc(N(C)CCO)cc23)CC1 | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL4470647 | 172063 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 446 | 7 | 1 | 6 | 4.7 | COc1ccccc1C1CCN(c2nc(C3CCC3)nc3ccc(N(C)CCO)cc23)CC1 | 10.1021/acs.jmedchem.9b00340 | ||
| 118610470 | 170809 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 464 | 8 | 0 | 6 | 5.1 | COCCN(C)c1ccc2nc(C3(F)CC3)nc(N3CCC(c4ccccc4OC)CC3)c2c1 | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL4451959 | 170809 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 464 | 8 | 0 | 6 | 5.1 | COCCN(C)c1ccc2nc(C3(F)CC3)nc(N3CCC(c4ccccc4OC)CC3)c2c1 | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL3622803 | 214342 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assayAgonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assay |
ChEMBL | None | None | None | C[Si](C)(C)C[C@H](NC(=O)[C@H](C[Si](C)(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCCN)C(=O)O | 10.1021/acs.jmedchem.5b00841 | ||||
| 90237648 | 176279 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 446 | 8 | 0 | 6 | 5.0 | COCCN(C)c1ccc2nc(C3CC3)nc(N3CCC(c4ccccc4OC)CC3)c2c1 | 10.1021/acs.jmedchem.9b00340 | ||
| CHEMBL4593175 | 176279 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assayAllosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay |
ChEMBL | 446 | 8 | 0 | 6 | 5.0 | COCCN(C)c1ccc2nc(C3CC3)nc(N3CCC(c4ccccc4OC)CC3)c2c1 | 10.1021/acs.jmedchem.9b00340 | ||
| 51035368 | 92520 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assayAgonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay |
ChEMBL | 404 | 5 | 0 | 6 | 4.2 | COc1cc2nc(C3CCC3)nc(N3CCN(c4ccccc4)CC3)c2cc1OC | 10.1021/ml400176n | ||
Showing 1 to 50 of 1,243 entries