Ligand source activities (1 row/activity)



Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
2139 3855 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 56 None 1 3 Mouse 9.0 pEC50 = 9 Functional
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 211811 0 None - 1 Mouse 6.0 pEC50 = 6 Functional
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 122572 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
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 122572 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
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 138719 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
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 138719 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
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 138793 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
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 138793 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
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 138879 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
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 138879 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
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 212448 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 122571 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
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 122571 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
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 138767 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
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 138767 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
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 122380 0 None - 1 Mouse 6.8 pEC50 = 6.8 Functional
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 122380 0 None - 1 Mouse 6.8 pEC50 = 6.8 Functional
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 122382 0 None - 1 Mouse 5.8 pEC50 = 5.8 Functional
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 122382 0 None - 1 Mouse 5.8 pEC50 = 5.8 Functional
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 138740 0 None - 1 Mouse 4.8 pEC50 = 4.8 Functional
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 138740 0 None - 1 Mouse 4.8 pEC50 = 4.8 Functional
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 122381 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
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 122381 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
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 138789 0 None - 1 Mouse 6.8 pEC50 = 6.8 Functional
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 138789 0 None - 1 Mouse 6.8 pEC50 = 6.8 Functional
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 212423 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 138719 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
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 138719 0 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
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 122383 0 None - 1 Mouse 4.7 pEC50 = 4.7 Functional
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 122383 0 None - 1 Mouse 4.7 pEC50 = 4.7 Functional
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 138736 0 None - 1 Mouse 5.6 pEC50 = 5.6 Functional
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 138736 0 None - 1 Mouse 5.6 pEC50 = 5.6 Functional
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 138789 0 None - 1 Mouse 6.6 pEC50 = 6.6 Functional
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 138789 0 None - 1 Mouse 6.6 pEC50 = 6.6 Functional
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 122385 0 None - 1 Mouse 5.6 pEC50 = 5.6 Functional
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 122385 0 None - 1 Mouse 5.6 pEC50 = 5.6 Functional
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 138740 0 None - 1 Mouse 4.6 pEC50 = 4.6 Functional
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
CHEMBL3780248 138740 0 None - 1 Mouse 4.6 pEC50 = 4.6 Functional
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
127032876 138861 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
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 578 8 3 6 0.3 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1 10.1016/j.ejmech.2016.01.038
CHEMBL3781773 138861 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
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 578 8 3 6 0.3 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1 10.1016/j.ejmech.2016.01.038
127032878 138770 0 None - 1 Mouse 6.6 pEC50 = 6.6 Functional
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 628 6 3 6 -0.6 Cn1c(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
CHEMBL3780633 138770 0 None - 1 Mouse 6.6 pEC50 = 6.6 Functional
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 628 6 3 6 -0.6 Cn1c(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
127032259 138783 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
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 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 138783 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
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 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
122185154 122570 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 450 6 4 7 -0.6 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1nccnc1N 10.1016/j.bmc.2015.07.022
CHEMBL3601782 122570 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 450 6 4 7 -0.6 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1nccnc1N 10.1016/j.bmc.2015.07.022
2139 3855 56 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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 None 10.1016/j.bmc.2006.09.045
2316 3855 56 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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 None 10.1016/j.bmc.2006.09.045
3836 3855 56 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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 None 10.1016/j.bmc.2006.09.045
638678 3855 56 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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 None 10.1016/j.bmc.2006.09.045
CHEMBL1472 3855 56 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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 None 10.1016/j.bmc.2006.09.045
DB09421 3855 56 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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 None 10.1016/j.bmc.2006.09.045
2139 3855 56 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
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 None None None None 10.1016/j.ejmech.2016.01.038
2316 3855 56 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
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 None None None None 10.1016/j.ejmech.2016.01.038
3836 3855 56 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
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 None None None None 10.1016/j.ejmech.2016.01.038
638678 3855 56 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
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 None None None None 10.1016/j.ejmech.2016.01.038
CHEMBL1472 3855 56 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
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 None None None None 10.1016/j.ejmech.2016.01.038
DB09421 3855 56 None 1 3 Mouse 8.5 pEC50 = 8.5 Functional
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 None None None None 10.1016/j.ejmech.2016.01.038
127032259 138783 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
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 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 138783 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
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 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
127032563 138772 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
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 502 6 3 6 -1.2 Cn1cc(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
CHEMBL3780645 138772 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
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 502 6 3 6 -1.2 Cn1cc(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
127032261 138751 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
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 482 8 3 6 -0.2 CCCn1cc(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
CHEMBL3780373 138751 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
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 482 8 3 6 -0.2 CCCn1cc(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
127032257 138846 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 410 6 3 6 -1.1 Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl 10.1016/j.ejmech.2016.01.038
CHEMBL3781522 138846 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 410 6 3 6 -1.1 Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl 10.1016/j.ejmech.2016.01.038
127032876 138861 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 578 8 3 6 0.3 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1 10.1016/j.ejmech.2016.01.038
CHEMBL3781773 138861 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 578 8 3 6 0.3 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1 10.1016/j.ejmech.2016.01.038
122185157 122573 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 449 6 2 7 -0.2 Cn1cnc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1Br 10.1016/j.bmc.2015.07.022
CHEMBL3601785 122573 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
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 449 6 2 7 -0.2 Cn1cnc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1Br 10.1016/j.bmc.2015.07.022
127032878 138770 0 None - 1 Mouse 4.4 pEC50 = 4.4 Functional
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 628 6 3 6 -0.6 Cn1c(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
CHEMBL3780633 138770 0 None - 1 Mouse 4.4 pEC50 = 4.4 Functional
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 628 6 3 6 -0.6 Cn1c(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
CHEMBL224525 209448 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 CCCc1nc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 10.1016/j.bmc.2006.09.045
122184252 122384 0 None - 1 Mouse 5.4 pEC50 = 5.4 Functional
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 435 6 3 6 -0.2 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1cnccn1 10.1016/j.bmc.2015.07.022
CHEMBL3600452 122384 0 None - 1 Mouse 5.4 pEC50 = 5.4 Functional
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 435 6 3 6 -0.2 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1cnccn1 10.1016/j.bmc.2015.07.022
CHEMBL223972 209447 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 Cn1cnc(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
127032875 138879 0 None - 1 Mouse 8.3 pEC50 = 8.3 Functional
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 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 138879 0 None - 1 Mouse 8.3 pEC50 = 8.3 Functional
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 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
122185153 122569 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
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 449 6 3 6 0.1 Cc1cnc(C(=O)N[C@@H](Cc2nc[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1 10.1016/j.bmc.2015.07.022
CHEMBL3601781 122569 0 None - 1 Mouse 6.3 pEC50 = 6.3 Functional
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 449 6 3 6 0.1 Cc1cnc(C(=O)N[C@@H](Cc2nc[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1 10.1016/j.bmc.2015.07.022
44422122 85112 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 514 9 5 7 -2.8 C[n+]1c[nH]cc1C[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 10.1016/j.bmc.2006.09.045
CHEMBL224730 85112 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 514 9 5 7 -2.8 C[n+]1c[nH]cc1C[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 10.1016/j.bmc.2006.09.045
127032563 138772 0 None - 1 Mouse 8.2 pEC50 = 8.2 Functional
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 502 6 3 6 -1.2 Cn1cc(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
CHEMBL3780645 138772 0 None - 1 Mouse 8.2 pEC50 = 8.2 Functional
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 502 6 3 6 -1.2 Cn1cc(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
CHEMBL388528 212418 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 C=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
127033489 138767 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
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 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 138767 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
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 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
127032877 138793 0 None - 1 Mouse 5.2 pEC50 = 5.2 Functional
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 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 138793 0 None - 1 Mouse 5.2 pEC50 = 5.2 Functional
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 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
122185158 122574 0 None - 1 Mouse 5.1 pEC50 = 5.1 Functional
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 637 7 2 7 0.7 CCn1c(I)nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1I 10.1016/j.bmc.2015.07.022
CHEMBL3601786 122574 0 None - 1 Mouse 5.1 pEC50 = 5.1 Functional
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 637 7 2 7 0.7 CCn1c(I)nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1I 10.1016/j.bmc.2015.07.022
122184244 122378 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
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 713 8 2 7 2.1 Cc1cnc(C(=O)N[C@@H](Cc2nc(I)n(Cc3ccccc3)c2I)C(=O)N2CCC[C@H]2C(N)=O)cn1 10.1016/j.bmc.2015.07.022
CHEMBL3600444 122378 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
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 713 8 2 7 2.1 Cc1cnc(C(=O)N[C@@H](Cc2nc(I)n(Cc3ccccc3)c2I)C(=O)N2CCC[C@H]2C(N)=O)cn1 10.1016/j.bmc.2015.07.022
122184254 122386 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
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 527 6 3 6 0.9 Cc1cnc(C(=O)N[C@@H](Cc2nc(Br)[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1 10.1016/j.bmc.2015.07.022
CHEMBL3600454 122386 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
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 527 6 3 6 0.9 Cc1cnc(C(=O)N[C@@H](Cc2nc(Br)[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1 10.1016/j.bmc.2015.07.022
127033192 138736 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
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 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 138736 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
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 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
127032257 138846 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
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 410 6 3 6 -1.1 Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl 10.1016/j.ejmech.2016.01.038
CHEMBL3781522 138846 0 None - 1 Mouse 6.1 pEC50 = 6.1 Functional
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 410 6 3 6 -1.1 Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl 10.1016/j.ejmech.2016.01.038
CHEMBL3600449 211810 0 None - 1 Mouse 6.0 pEC50 = 6.0 Functional
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 CCCc1nc(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
122184245 122379 0 None - 1 Mouse 6.0 pEC50 = 6.0 Functional
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 699 8 2 7 1.7 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)c1cnccn1 10.1016/j.bmc.2015.07.022
CHEMBL3600445 122379 0 None - 1 Mouse 6.0 pEC50 = 6.0 Functional
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 699 8 2 7 1.7 NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)c1cnccn1 10.1016/j.bmc.2015.07.022


Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
2139 3855 56 None -1 4 Mouse 9.3 pEC50 = 9.3 Binding
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 56 None -1 4 Mouse 9.3 pEC50 = 9.3 Binding
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 56 None -1 4 Mouse 9.3 pEC50 = 9.3 Binding
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 56 None -1 4 Mouse 9.3 pEC50 = 9.3 Binding
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 56 None -1 4 Mouse 9.3 pEC50 = 9.3 Binding
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 56 None -1 4 Mouse 9.3 pEC50 = 9.3 Binding
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 127224 0 None - 1 Rat 9.3 pEC50 = 9.3 Binding
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 127224 0 None - 1 Rat 9.3 pEC50 = 9.3 Binding
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 56 None -1 4 Mouse 9.2 pEC50 = 9.2 Binding
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 56 None -1 4 Mouse 9.2 pEC50 = 9.2 Binding
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 56 None -1 4 Mouse 9.2 pEC50 = 9.2 Binding
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 56 None -1 4 Mouse 9.2 pEC50 = 9.2 Binding
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 56 None -1 4 Mouse 9.2 pEC50 = 9.2 Binding
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 56 None -1 4 Mouse 9.2 pEC50 = 9.2 Binding
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 212048 14 None - 1 Mouse 7.0 pEC50 = 7.0 Binding
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 5416 1 None - 1 Mouse 5.8 pEC50 = 5.8 Binding
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 5416 1 None - 1 Mouse 5.8 pEC50 = 5.8 Binding
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 108453 1 None - 1 Mouse 4.8 pEC50 = 4.8 Binding
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 108453 1 None - 1 Mouse 4.8 pEC50 = 4.8 Binding
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 201858 0 None - 1 Mouse 6.5 pEC50 = 6.5 Binding
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 201858 0 None - 1 Mouse 6.5 pEC50 = 6.5 Binding
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 209105 0 None - 1 Rat 6.5 pEC50 = 6.5 Binding
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 56 None -2 4 Rat 8.5 pEC50 = 8.5 Binding
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 56 None -2 4 Rat 8.5 pEC50 = 8.5 Binding
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 56 None -2 4 Rat 8.5 pEC50 = 8.5 Binding
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 56 None -2 4 Rat 8.5 pEC50 = 8.5 Binding
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 56 None -2 4 Rat 8.5 pEC50 = 8.5 Binding
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 56 None -2 4 Rat 8.5 pEC50 = 8.5 Binding
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 209843 3 None - 1 Mouse 6.4 pEC50 = 6.4 Binding
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 138879 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
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 138879 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
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 138783 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
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 138783 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
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 138719 0 None - 0 Mouse 4.7 pIC50 = 4.7 Binding
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 138719 0 None - 0 Mouse 4.7 pIC50 = 4.7 Binding
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 56 None -1 4 Mouse 8.6 pIC50 = 8.6 Binding
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 56 None -1 4 Mouse 8.6 pIC50 = 8.6 Binding
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 56 None -1 4 Mouse 8.6 pIC50 = 8.6 Binding
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 56 None -1 4 Mouse 8.6 pIC50 = 8.6 Binding
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 56 None -1 4 Mouse 8.6 pIC50 = 8.6 Binding
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 56 None -1 4 Mouse 8.6 pIC50 = 8.6 Binding
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 138740 0 None - 0 Mouse 4.7 pIC50 = 4.7 Binding
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 138740 0 None - 0 Mouse 4.7 pIC50 = 4.7 Binding
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 56 None -1 4 Mouse 7.6 pIC50 = 7.6 Binding
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 56 None -1 4 Mouse 7.6 pIC50 = 7.6 Binding
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 56 None -1 4 Mouse 7.6 pIC50 = 7.6 Binding
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
638678 3855 56 None -1 4 Mouse 7.6 pIC50 = 7.6 Binding
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
CHEMBL1472 3855 56 None -1 4 Mouse 7.6 pIC50 = 7.6 Binding
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
DB09421 3855 56 None -1 4 Mouse 7.6 pIC50 = 7.6 Binding
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
127033191 138789 0 None - 0 Mouse 4.5 pIC50 = 4.5 Binding
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 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 138789 0 None - 0 Mouse 4.5 pIC50 = 4.5 Binding
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 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
127032563 138772 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
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 502 6 3 6 -1.2 Cn1cc(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
CHEMBL3780645 138772 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
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 502 6 3 6 -1.2 Cn1cc(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
127032878 138770 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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 628 6 3 6 -0.6 Cn1c(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
CHEMBL3780633 138770 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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 628 6 3 6 -0.6 Cn1c(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
CHEMBL39363 212468 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None Cn1cnc(C[C@H](NC(=O)[C@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1 10.1021/jm960053k
2139 3855 56 None -1 4 Mouse 8.0 pKi = 8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None None 10.1021/jm960053k
2316 3855 56 None -1 4 Mouse 8.0 pKi = 8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None None 10.1021/jm960053k
3836 3855 56 None -1 4 Mouse 8.0 pKi = 8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None None 10.1021/jm960053k
638678 3855 56 None -1 4 Mouse 8.0 pKi = 8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None None 10.1021/jm960053k
CHEMBL1472 3855 56 None -1 4 Mouse 8.0 pKi = 8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None None 10.1021/jm960053k
DB09421 3855 56 None -1 4 Mouse 8.0 pKi = 8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
ChEMBL None None None None 10.1021/jm960053k
CHEMBL390942 212448 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
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
9979181 5416 1 None - 1 Mouse 5.8 pKi = 5.8 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
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 5416 1 None - 1 Mouse 5.8 pKi = 5.8 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
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
CHEMBL36631 212048 14 None - 1 Mouse 5.8 pKi = 5.8 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against 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
2139 3855 56 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None None 10.1016/j.bmc.2006.09.045
2316 3855 56 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None None 10.1016/j.bmc.2006.09.045
3836 3855 56 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None None 10.1016/j.bmc.2006.09.045
638678 3855 56 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None None 10.1016/j.bmc.2006.09.045
CHEMBL1472 3855 56 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None None 10.1016/j.bmc.2006.09.045
DB09421 3855 56 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None None 10.1016/j.bmc.2006.09.045
2139 3855 56 None -2 4 Rat 7.7 pKi = 7.7 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
ChEMBL None None None None 10.1021/jm0505462
2316 3855 56 None -2 4 Rat 7.7 pKi = 7.7 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
ChEMBL None None None None 10.1021/jm0505462
3836 3855 56 None -2 4 Rat 7.7 pKi = 7.7 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
ChEMBL None None None None 10.1021/jm0505462
638678 3855 56 None -2 4 Rat 7.7 pKi = 7.7 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
ChEMBL None None None None 10.1021/jm0505462
CHEMBL1472 3855 56 None -2 4 Rat 7.7 pKi = 7.7 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
ChEMBL None None None None 10.1021/jm0505462
DB09421 3855 56 None -2 4 Rat 7.7 pKi = 7.7 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
ChEMBL None None None None 10.1021/jm0505462
134134558 143358 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes
ChEMBL 518 11 3 5 4.9 O=C(O)C(Cc1ccccc1)N[C@@H](Cc1cn(Cc2ccccc2)cn1)C(=O)Nc1ccc2ccccc2c1 nan
CHEMBL3897627 143358 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes
ChEMBL 518 11 3 5 4.9 O=C(O)C(Cc1ccccc1)N[C@@H](Cc1cn(Cc2ccccc2)cn1)C(=O)Nc1ccc2ccccc2c1 nan
2139 3855 56 None -1 4 Mouse 7.6 pKi = 7.6 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
ChEMBL None None None None 10.1016/s0960-894x(98)00567-8
2316 3855 56 None -1 4 Mouse 7.6 pKi = 7.6 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
ChEMBL None None None None 10.1016/s0960-894x(98)00567-8
3836 3855 56 None -1 4 Mouse 7.6 pKi = 7.6 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
ChEMBL None None None None 10.1016/s0960-894x(98)00567-8
638678 3855 56 None -1 4 Mouse 7.6 pKi = 7.6 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
ChEMBL None None None None 10.1016/s0960-894x(98)00567-8
CHEMBL1472 3855 56 None -1 4 Mouse 7.6 pKi = 7.6 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
ChEMBL None None None None 10.1016/s0960-894x(98)00567-8
DB09421 3855 56 None -1 4 Mouse 7.6 pKi = 7.6 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
ChEMBL None None None None 10.1016/s0960-894x(98)00567-8
44422122 85112 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL 514 9 5 7 -2.8 C[n+]1c[nH]cc1C[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 10.1016/j.bmc.2006.09.045
CHEMBL224730 85112 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL 514 9 5 7 -2.8 C[n+]1c[nH]cc1C[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 10.1016/j.bmc.2006.09.045
44403976 127224 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRHInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH
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 127224 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRHInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH
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
CHEMBL223972 209447 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None Cn1cnc(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
CHEMBL197149 209105 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.27-0.37 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.27-0.37 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
9979180 108453 1 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
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 108453 1 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
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
CHEMBL224525 209448 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None CCCc1nc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 10.1016/j.bmc.2006.09.045
2139 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain
ChEMBL None None None None 10.1021/jm020531t
2316 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain
ChEMBL None None None None 10.1021/jm020531t
3836 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain
ChEMBL None None None None 10.1021/jm020531t
638678 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain
ChEMBL None None None None 10.1021/jm020531t
CHEMBL1472 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain
ChEMBL None None None None 10.1021/jm020531t
DB09421 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain
ChEMBL None None None None 10.1021/jm020531t
11795153 201858 0 None - 1 Mouse 5.4 pKi = 5.4 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against 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 201858 0 None - 1 Mouse 5.4 pKi = 5.4 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against 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
10255308 144435 0 None - 1 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes
ChEMBL 497 7 4 7 -0.3 Cc1cc(=O)oc2cc(NC(=O)[C@@H]3CCCN3C(=O)[C@H](CC(N)=O)NC(=O)[C@@H]3CCC(=O)N3)ccc12 nan
CHEMBL3906398 144435 0 None - 1 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes
ChEMBL 497 7 4 7 -0.3 Cc1cc(=O)oc2cc(NC(=O)[C@@H]3CCCN3C(=O)[C@H](CC(N)=O)NC(=O)[C@@H]3CCC(=O)N3)ccc12 nan
CHEMBL2370383 209843 3 None - 1 Mouse 5.2 pKi = 5.2 Binding
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using 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 10.1016/s0960-894x(98)00567-8
CHEMBL3954284 212486 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes
ChEMBL None None None NC(=O)C[C@H](NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(N)=O nan
CHEMBL388528 212418 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
ChEMBL None None None C=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
2137 2521 0 None -1 2 Rat 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 3 5 -1.5 O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1 6264336
2141 2521 0 None -1 2 Rat 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 3 5 -1.5 O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1 6264336
5311291 2521 0 None -1 2 Rat 8.5 pKd = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 3 5 -1.5 O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1 6264336
None 216337 0 3H-MeTRH 1 2 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 362 6 4 5 -1.8 C1CC(N(C1)C(=O)C(CC2=CN=CN2)NC(=O)C3CCC(=O)N3)C(=O)N None
None 216337 0 3H-MeTRH -1 2 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 362 6 4 5 -1.8 C1CC(N(C1)C(=O)C(CC2=CN=CN2)NC(=O)C3CCC(=O)N3)C(=O)N None
None 216337 0 3H-N tau (1)-Me-His-TRH -1 2 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 362 6 4 5 -1.8 C1CC(N(C1)C(=O)C(CC2=CN=CN2)NC(=O)C3CCC(=O)N3)C(=O)N None
2712 916 34 None -45 4 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
3370 916 34 None -45 4 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
594 916 34 None -45 4 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
CHEMBL451 916 34 None -45 4 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
DB00475 916 34 None -45 4 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
2712 916 34 None -40 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
3370 916 34 None -40 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
594 916 34 None -40 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
CHEMBL451 916 34 None -40 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
DB00475 916 34 None -40 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
3016 1412 48 None -46 5 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
3364 1412 48 None -46 5 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
852 1412 48 None -46 5 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
CHEMBL12 1412 48 None -46 5 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
DB00829 1412 48 None -46 5 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
1802 2533 33 None 1513 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F None
3342 2533 33 None 1513 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F None
4192 2533 33 None 1513 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F None
CHEMBL655 2533 33 None 1513 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F None
DB00683 2533 33 None 1513 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F None
114750 3746 0 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 405 6 4 6 -2.1 CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1 None
2143 3746 0 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 405 6 4 6 -2.1 CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1 None
CHEMBL2107016 3746 0 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 405 6 4 6 -2.1 CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1 None
2712 916 34 None 5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
3370 916 34 None 5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
594 916 34 None 5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
CHEMBL451 916 34 None 5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
DB00475 916 34 None 5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
2139 3855 56 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
Drug Central None None None None None
2316 3855 56 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
Drug Central None None None None None
3836 3855 56 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
Drug Central None None None None None
638678 3855 56 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
Drug Central None None None None None
CHEMBL1472 3855 56 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
Drug Central None None None None None
DB09421 3855 56 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1
Drug Central None None None None None
2139 3855 56 None -2 4 Rat 8.1 pKi = 8.1 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
Drug Central None None None None None
2316 3855 56 None -2 4 Rat 8.1 pKi = 8.1 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
Drug Central None None None None None
3836 3855 56 None -2 4 Rat 8.1 pKi = 8.1 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
Drug Central None None None None None
638678 3855 56 None -2 4 Rat 8.1 pKi = 8.1 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
Drug Central None None None None None
CHEMBL1472 3855 56 None -2 4 Rat 8.1 pKi = 8.1 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
Drug Central None None None None None
DB09421 3855 56 None -2 4 Rat 8.1 pKi = 8.1 Binding
Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM
Drug Central None None None None None
2139 3855 56 None -1 4 Mouse 8.1 pKi = 8.1 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
Drug Central None None None None None
2316 3855 56 None -1 4 Mouse 8.1 pKi = 8.1 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
Drug Central None None None None None
3836 3855 56 None -1 4 Mouse 8.1 pKi = 8.1 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
Drug Central None None None None None
638678 3855 56 None -1 4 Mouse 8.1 pKi = 8.1 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
Drug Central None None None None None
CHEMBL1472 3855 56 None -1 4 Mouse 8.1 pKi = 8.1 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
Drug Central None None None None None
DB09421 3855 56 None -1 4 Mouse 8.1 pKi = 8.1 Binding
Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
Drug Central None None None None None
2712 916 34 None -45 4 Mouse 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2175902
3370 916 34 None -45 4 Mouse 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2175902
594 916 34 None -45 4 Mouse 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2175902
CHEMBL451 916 34 None -45 4 Mouse 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2175902
DB00475 916 34 None -45 4 Mouse 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2175902
2712 916 34 None -40 4 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2566295
3370 916 34 None -40 4 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2566295
594 916 34 None -40 4 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2566295
CHEMBL451 916 34 None -40 4 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2566295
DB00475 916 34 None -40 4 Rat 4.8 pKi = 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 2566295
3016 1412 48 None -46 5 Rat 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 2566295
3364 1412 48 None -46 5 Rat 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 2566295
852 1412 48 None -46 5 Rat 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 2566295
CHEMBL12 1412 48 None -46 5 Rat 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 2566295
DB00829 1412 48 None -46 5 Rat 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 2566295
1802 2533 33 None 1513 2 Rat 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 2566295
3342 2533 33 None 1513 2 Rat 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 2566295
4192 2533 33 None 1513 2 Rat 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 2566295
CHEMBL655 2533 33 None 1513 2 Rat 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 2566295
DB00683 2533 33 None 1513 2 Rat 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 1 0 3 4.3 Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F 2566295
114750 3746 0 None - 1 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 405 6 4 6 -2.1 CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1 23087672
2143 3746 0 None - 1 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 405 6 4 6 -2.1 CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1 23087672
CHEMBL2107016 3746 0 None - 1 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 405 6 4 6 -2.1 CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1 23087672
2139 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
2316 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
3836 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
638678 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
CHEMBL1472 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
DB09421 3855 56 None -2 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
2137 2521 0 None 1 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 3 5 -1.5 O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1 5001013
2141 2521 0 None 1 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 3 5 -1.5 O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1 5001013
5311291 2521 0 None 1 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 3 5 -1.5 O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1 5001013