Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
2139 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 210064 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 122057 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 122057 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 138190 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 138190 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 138264 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 138264 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 138350 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 138350 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 210701 0 None -5 2 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 122056 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 122056 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 138238 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 138238 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 121865 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 121865 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 121867 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 121867 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 138211 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 138211 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 121866 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 121866 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 138260 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 138260 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 210676 0 None -8 2 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 138190 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 138190 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 121868 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 121868 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 138207 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 138207 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 138260 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 138260 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 121870 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 121870 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 138211 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 138211 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 138332 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 138332 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 138241 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 138241 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 138254 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 138254 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 122055 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 122055 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 138254 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 138254 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 138243 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 138243 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 138222 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 138222 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 138317 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 138317 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 138332 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 138332 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 122058 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 122058 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 138241 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 138241 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 207703 0 None -13 2 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 121869 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 121869 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 207702 0 None -2 2 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 138350 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 138350 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 122054 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 122054 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 84688 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 84688 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 138243 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 138243 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 210671 0 None -15 2 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 138238 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 138238 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 138264 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 138264 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 122059 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 122059 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 121863 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 121863 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 121871 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 121871 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 138207 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 138207 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 138317 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 138317 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 210063 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 121864 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 121864 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




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
2139 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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
2139 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 210301 11 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 5344 0 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 5344 0 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 107967 0 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 107967 0 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 200173 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 200173 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
CHEMBL2370383 208098 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 138350 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 138350 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 138254 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 138254 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 138190 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 138190 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 138211 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 138211 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 138260 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 138260 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 138243 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 138243 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 138241 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 138241 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 210721 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 210701 0 None 3 2 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 5344 0 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 5344 0 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 210301 11 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 84688 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 84688 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
CHEMBL223972 207702 0 None 3 2 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
9979180 107967 0 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 107967 0 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 207703 0 None -1 2 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
11795153 200173 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 200173 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
CHEMBL2370383 208098 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
CHEMBL388528 210671 0 None 2 2 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 2485 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 2485 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 2485 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 214586 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 214586 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 214586 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 903 33 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 903 33 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
594 903 33 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 903 33 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 903 33 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 903 33 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 903 33 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
594 903 33 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 903 33 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 903 33 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 1385 0 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 1385 0 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 1385 0 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 1385 0 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 1385 0 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 2497 0 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 2497 0 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 2497 0 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 2497 0 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 2497 0 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 3689 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 3689 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 3689 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 903 33 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 903 33 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
594 903 33 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 903 33 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 903 33 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 None -1 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 3794 51 None -1 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 3794 51 None -1 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 3794 51 None -1 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 3794 51 None -1 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 3794 51 None -1 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 3794 51 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 903 33 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 903 33 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
594 903 33 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 903 33 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 903 33 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 903 33 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 903 33 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
594 903 33 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 903 33 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 903 33 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 1385 0 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 1385 0 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 1385 0 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 1385 0 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 1385 0 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 2497 0 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 2497 0 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 2497 0 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 2497 0 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 2497 0 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 3689 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 3689 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 3689 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 3794 51 None -1 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
2316 3794 51 None -1 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
3836 3794 51 None -1 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
638678 3794 51 None -1 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
CHEMBL1472 3794 51 None -1 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
DB09421 3794 51 None -1 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8592728
2137 2485 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 2485 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 2485 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