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
1146 10634 56 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse TAAR5 expressed in HEK293 cells assessed as increase in cAMP release after 30 mins by BRET assay relative to controlAgonist activity at mouse TAAR5 expressed in HEK293 cells assessed as increase in cAMP release after 30 mins by BRET assay relative to control
ChEMBL 59 0 0 1 0.2 CN(C)C 10.1039/C5MD00490J
5521 10634 56 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse TAAR5 expressed in HEK293 cells assessed as increase in cAMP release after 30 mins by BRET assay relative to controlAgonist activity at mouse TAAR5 expressed in HEK293 cells assessed as increase in cAMP release after 30 mins by BRET assay relative to control
ChEMBL 59 0 0 1 0.2 CN(C)C 10.1039/C5MD00490J
CHEMBL439723 10634 56 None - 1 Mouse 5.7 pEC50 = 5.7 Functional
Agonist activity at mouse TAAR5 expressed in HEK293 cells assessed as increase in cAMP release after 30 mins by BRET assay relative to controlAgonist activity at mouse TAAR5 expressed in HEK293 cells assessed as increase in cAMP release after 30 mins by BRET assay relative to control
ChEMBL 59 0 0 1 0.2 CN(C)C 10.1039/C5MD00490J
56946474 78291 0 None - 1 Mouse 4.5 pIC50 = 4.5 Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assayAntagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
ChEMBL 403 9 1 4 4.8 COc1ccccc1OCCNCC1CCC(c2ccccc2)(c2ccccc2)O1 10.1039/C5MD00490J
CHEMBL1946779 78291 0 None - 1 Mouse 4.5 pIC50 = 4.5 Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assayAntagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
ChEMBL 403 9 1 4 4.8 COc1ccccc1OCCNCC1CCC(c2ccccc2)(c2ccccc2)O1 10.1039/C5MD00490J
CHEMBL1962769 78291 0 None - 1 Mouse 4.5 pIC50 = 4.5 Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assayAntagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
ChEMBL 403 9 1 4 4.8 COc1ccccc1OCCNCC1CCC(c2ccccc2)(c2ccccc2)O1 10.1039/C5MD00490J
56946573 78301 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assayAntagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
ChEMBL 428 6 0 4 4.9 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1039/C5MD00490J
CHEMBL1946780 78301 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assayAntagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
ChEMBL 428 6 0 4 4.9 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1039/C5MD00490J
CHEMBL1962870 78301 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assayAntagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
ChEMBL 428 6 0 4 4.9 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1039/C5MD00490J
11723 8207 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 73 1 0 1 0.6 CCN(C)C 17088868
5523 8207 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 73 1 0 1 0.6 CCN(C)C 17088868
CHEMBL609099 8207 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 73 1 0 1 0.6 CCN(C)C 17088868
1146 10634 56 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 59 0 0 1 0.2 CN(C)C 16878137
5521 10634 56 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 59 0 0 1 0.2 CN(C)C 16878137
CHEMBL439723 10634 56 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 59 0 0 1 0.2 CN(C)C 16878137




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
9950514 18630 13 None - 0 Human 5.4 pEC50 = 5.4 Binding
Inverse agonist activity at human TAAR5 expressed in HEK293 cells by Alphascreen assayInverse agonist activity at human TAAR5 expressed in HEK293 cells by Alphascreen assay
ChEMBL 355 4 2 3 3.3 NCCc1ccc(Oc2ccc(O)cc2)c(I)c1 10.1039/C5MD00490J
CHEMBL1182312 18630 13 None - 0 Human 5.4 pEC50 = 5.4 Binding
Inverse agonist activity at human TAAR5 expressed in HEK293 cells by Alphascreen assayInverse agonist activity at human TAAR5 expressed in HEK293 cells by Alphascreen assay
ChEMBL 355 4 2 3 3.3 NCCc1ccc(Oc2ccc(O)cc2)c(I)c1 10.1039/C5MD00490J
CHEMBL229288 18630 13 None - 0 Human 5.4 pEC50 = 5.4 Binding
Inverse agonist activity at human TAAR5 expressed in HEK293 cells by Alphascreen assayInverse agonist activity at human TAAR5 expressed in HEK293 cells by Alphascreen assay
ChEMBL 355 4 2 3 3.3 NCCc1ccc(Oc2ccc(O)cc2)c(I)c1 10.1039/C5MD00490J