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
| |
| 2139 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 2316 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 3836 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 638678 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 638678.0 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| CHEMBL1472 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| DB09421 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 2139 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 2316 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 3836 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 638678 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 638678.0 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| CHEMBL1472 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| DB09421 | 3855 | None | 43 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 1 | 3 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| CHEMBL3600450 | 214271 | None | 0 | Mouse | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | None | None | None | CC(C)c1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||||
| 122185156 | 122638 | None | 0 | Mouse | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 609 | 6 | 3 | 6 | 0.2 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)[nH]c1I)NC(=O)c1cnccn1 | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3601784 | 122638 | None | 0 | Mouse | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 609 | 6 | 3 | 6 | 0.2 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)[nH]c1I)NC(=O)c1cnccn1 | 10.1016/j.bmc.2015.07.022 | ||
| 127032260 | 138806 | None | 0 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 468 | 7 | 3 | 6 | -0.6 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3779931 | 138806 | None | 0 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 468 | 7 | 3 | 6 | -0.6 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| 127032877 | 138880 | None | 0 | Mouse | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 430 | 6 | 4 | 5 | -0.5 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780836 | 138880 | None | 0 | Mouse | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 430 | 6 | 4 | 5 | -0.5 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| 127032875 | 138966 | None | 0 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 516 | 7 | 3 | 6 | -0.7 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3782037 | 138966 | None | 0 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 516 | 7 | 3 | 6 | -0.7 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL390942 | 214908 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity |
ChEMBL | None | None | None | CCn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1 | 10.1016/j.bmc.2006.09.045 | ||||
| 122185155 | 122637 | None | 0 | Mouse | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 528 | 6 | 4 | 7 | 0.1 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1nccnc1N | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3601783 | 122637 | None | 0 | Mouse | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 528 | 6 | 4 | 7 | 0.1 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1nccnc1N | 10.1016/j.bmc.2015.07.022 | ||
| 127033489 | 138854 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 704 | 8 | 3 | 6 | 0.9 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780549 | 138854 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 704 | 8 | 3 | 6 | 0.9 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| 122184246 | 122446 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 399 | 8 | 3 | 6 | -0.0 | CCCc1nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3600446 | 122446 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 399 | 8 | 3 | 6 | -0.0 | CCCc1nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||
| 122184248 | 122448 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 414 | 8 | 4 | 7 | -0.4 | CCCc1nc(C[C@H](NC(=O)c2nccnc2N)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3600448 | 122448 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 414 | 8 | 4 | 7 | -0.4 | CCCc1nc(C[C@H](NC(=O)c2nccnc2N)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||
| 127032258 | 138827 | None | 0 | Mouse | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 486 | 8 | 3 | 6 | 0.4 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780248 | 138827 | None | 0 | Mouse | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 486 | 8 | 3 | 6 | 0.4 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| 122184247 | 122447 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 413 | 8 | 3 | 6 | 0.3 | CCCc1nc(C[C@H](NC(=O)c2cnc(C)cn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3600447 | 122447 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 413 | 8 | 3 | 6 | 0.3 | CCCc1nc(C[C@H](NC(=O)c2cnc(C)cn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1016/j.bmc.2015.07.022 | ||
| 127033191 | 138876 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 642 | 7 | 3 | 6 | -0.1 | CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780802 | 138876 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 642 | 7 | 3 | 6 | -0.1 | CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL389037 | 214883 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity |
ChEMBL | None | None | None | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)cn1)NC(=O)[C@@H]1CCCC(=O)N1 | 10.1016/j.bmc.2006.09.045 | ||||
| 127032260 | 138806 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 468 | 7 | 3 | 6 | -0.6 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3779931 | 138806 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA |
ChEMBL | 468 | 7 | 3 | 6 | -0.6 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| 122184251 | 122449 | None | 0 | Mouse | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 391 | 6 | 3 | 6 | -0.3 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Cl)NC(=O)c1cnccn1 | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3600451 | 122449 | None | 0 | Mouse | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 391 | 6 | 3 | 6 | -0.3 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Cl)NC(=O)c1cnccn1 | 10.1016/j.bmc.2015.07.022 | ||
| 127033192 | 138823 | None | 0 | Mouse | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 656 | 8 | 3 | 6 | 0.3 | CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780191 | 138823 | None | 0 | Mouse | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 656 | 8 | 3 | 6 | 0.3 | CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I | 10.1016/j.ejmech.2016.01.038 | ||
| 127033191 | 138876 | None | 0 | Mouse | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 642 | 7 | 3 | 6 | -0.1 | CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780802 | 138876 | None | 0 | Mouse | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 642 | 7 | 3 | 6 | -0.1 | CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I | 10.1016/j.ejmech.2016.01.038 | ||
| 122184253 | 122451 | None | 0 | Mouse | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 513 | 6 | 3 | 6 | 0.5 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1cnccn1 | 10.1016/j.bmc.2015.07.022 | ||
| CHEMBL3600453 | 122451 | None | 0 | Mouse | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method |
ChEMBL | 513 | 6 | 3 | 6 | 0.5 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1cnccn1 | 10.1016/j.bmc.2015.07.022 | ||
| 127032258 | 138827 | None | 0 | Mouse | Functional | pEC50 | = | 4.6 | 4.6 | - | 1 | Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay |
ChEMBL | 486 | 8 | 3 | 6 | 0.4 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
Showing 1 to 50 of 117 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
| |
| 2139 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| 2316 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| 3836 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| 638678 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| 638678.0 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| CHEMBL1472 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| DB09421 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.3 | 9.3 | -1 | 4 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | None | 10.1016/s0960-894x(98)00567-8 | ||||
| 44403976 | 127291 | None | 0 | Rat | Binding | pEC50 | = | 9.3 | 9.3 | - | 1 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8 |
ChEMBL | 513 | 9 | 4 | 9 | -2.3 | Cn1cncc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O | 10.1021/jm0505462 | ||
| CHEMBL365775 | 127291 | None | 0 | Rat | Binding | pEC50 | = | 9.3 | 9.3 | - | 1 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8 |
ChEMBL | 513 | 9 | 4 | 9 | -2.3 | Cn1cncc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O | 10.1021/jm0505462 | ||
| 2139 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| 2316 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| 3836 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| 638678 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| 638678.0 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| CHEMBL1472 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| DB09421 | 3855 | None | 43 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | -1 | 4 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | None | 10.1021/jm960053k | ||||
| CHEMBL36631 | 214508 | None | 11 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 1 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | None | None | None | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm960053k | ||||
| 9979181 | 5418 | None | 1 | Mouse | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | 414 | 3 | 2 | 4 | 1.0 | NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21 | 10.1016/s0960-894x(98)00567-8 | ||
| CHEMBL107238 | 5418 | None | 1 | Mouse | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | 414 | 3 | 2 | 4 | 1.0 | NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21 | 10.1016/s0960-894x(98)00567-8 | ||
| 9979180 | 108509 | None | 1 | Mouse | Binding | pEC50 | = | 4.8 | 4.8 | - | 1 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | 414 | 3 | 2 | 4 | 1.0 | NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12 | 10.1016/s0960-894x(98)00567-8 | ||
| CHEMBL319910 | 108509 | None | 1 | Mouse | Binding | pEC50 | = | 4.8 | 4.8 | - | 1 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | 414 | 3 | 2 | 4 | 1.0 | NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12 | 10.1016/s0960-894x(98)00567-8 | ||
| 11795153 | 204315 | None | 0 | Mouse | Binding | pEC50 | = | 6.5 | 6.5 | - | 1 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | 398 | 5 | 2 | 4 | -0.0 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O | 10.1021/jm960053k | ||
| CHEMBL607173 | 204315 | None | 0 | Mouse | Binding | pEC50 | = | 6.5 | 6.5 | - | 1 | Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells |
ChEMBL | 398 | 5 | 2 | 4 | -0.0 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O | 10.1021/jm960053k | ||
| CHEMBL197149 | 211564 | None | 0 | Rat | Binding | pEC50 | = | 6.5 | 6.5 | - | 1 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.16-0.51 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.16-0.51 uM |
ChEMBL | None | None | None | CCCc1nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 | 10.1021/jm0505462 | ||||
| 2139 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| 2316 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| 3836 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| 638678 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| 638678.0 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| CHEMBL1472 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| DB09421 | 3855 | None | 43 | Rat | Binding | pEC50 | = | 8.5 | 8.5 | -2 | 4 | Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM |
ChEMBL | None | None | None | None | 10.1021/jm0505462 | ||||
| CHEMBL2370383 | 212302 | None | 2 | Mouse | Binding | pEC50 | = | 6.4 | 6.4 | - | 1 | Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol |
ChEMBL | None | None | None | NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/s0960-894x(98)00567-8 | ||||
| 127032875 | 138966 | None | 0 | Mouse | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 516 | 7 | 3 | 6 | -0.7 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3782037 | 138966 | None | 0 | Mouse | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 516 | 7 | 3 | 6 | -0.7 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I | 10.1016/j.ejmech.2016.01.038 | ||
| 127032259 | 138870 | None | 0 | Mouse | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 454 | 6 | 3 | 6 | -1.0 | Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780746 | 138870 | None | 0 | Mouse | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 454 | 6 | 3 | 6 | -1.0 | Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| 127032260 | 138806 | None | 0 | Mouse | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 468 | 7 | 3 | 6 | -0.6 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3779931 | 138806 | None | 0 | Mouse | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 468 | 7 | 3 | 6 | -0.6 | CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br | 10.1016/j.ejmech.2016.01.038 | ||
| 2139 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 2316 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 3836 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 638678 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 638678.0 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| CHEMBL1472 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| DB09421 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 4 | Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method |
ChEMBL | None | None | None | None | 10.1016/j.bmc.2015.07.022 | ||||
| 127032258 | 138827 | None | 0 | Mouse | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 486 | 8 | 3 | 6 | 0.4 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| CHEMBL3780248 | 138827 | None | 0 | Mouse | Binding | pIC50 | = | 4.7 | 4.7 | - | 0 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | 486 | 8 | 3 | 6 | 0.4 | NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1016/j.ejmech.2016.01.038 | ||
| 2139 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 7.6 | 7.6 | -1 | 4 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 2316 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 7.6 | 7.6 | -1 | 4 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
| 3836 | 3855 | None | 43 | Mouse | Binding | pIC50 | = | 7.6 | 7.6 | -1 | 4 | Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs |
ChEMBL | None | None | None | None | 10.1016/j.ejmech.2016.01.038 | ||||
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