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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| CHEMBL2375494 | 89657 | None | 15 | Human | Binding | IC50 | = | 650.00 | 6.19 | - | 2 | Inhibition of GPR52 (unknown origin) | ChEMBL | 236.1 | 5 | 0 | 1 | 4.06 | O=C(/C=C/CCc1ccccc1)c1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.2c00799 | |
| CHEMBL240484 | 91578 | None | 20 | Human | Binding | IC50 | = | 5450.00 | 5.26 | - | 2 | Inhibition of GPR52 (unknown origin) | ChEMBL | 264.2 | 7 | 0 | 1 | 4.38 | O=C(/C=C/CCc1ccccc1)CCc1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.2c00799 | |
| CHEMBL3299117 | 112599 | None | 0 | Human | Binding | EC50 | = | 645.65 | 6.19 | - | 1 | Agonist activity at GPR52 (unknown origin) | ChEMBL | 430.1 | 8 | 2 | 4 | 4.11 | O=C(NCCO)c1cccc(-c2cccc(OCCc3cccc(C(F)(F)F)c3)n2)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299118 | 112600 | None | 0 | Human | Binding | EC50 | = | 346.74 | 6.46 | - | 1 | Agonist activity at GPR52 (unknown origin) | ChEMBL | 414.1 | 8 | 2 | 4 | 3.88 | O=C(NCCO)c1cccc(-c2cccc(OCCc3cc(F)cc(Cl)c3)n2)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL4782344 | 182254 | None | 23 | Human | Binding | IC50 | = | 630.00 | 6.20 | - | 2 | Inhibition of GPR52 (unknown origin) | ChEMBL | 242.1 | 5 | 0 | 2 | 4.12 | O=C(/C=C/CCc1ccccc1)c1cccs1 | https://dx.doi.org/10.1021/acs.jmedchem.2c00799 | |
| CHEMBL5267002 | 193611 | None | 0 | Human | Binding | EC50 | = | 630.96 | 6.20 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 391.1 | 3 | 1 | 5 | 2.70 | O=C1NCCc2c1nnn2-c1ccnc(Cc2cc(F)cc(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5271921 | 193811 | None | 0 | Human | Binding | EC50 | = | 63.10 | 7.20 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 372.1 | 3 | 1 | 4 | 3.16 | O=C1NCCc2c1cnn2-c1cc(Cc2cccc(C(F)(F)F)c2)ccn1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5272124 | 193817 | None | 0 | Human | Binding | EC50 | = | 251.19 | 6.60 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 376.1 | 3 | 1 | 4 | 3.26 | O=C1NCc2c1cnn2-c1ccnc(Cc2cc(F)cc(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5273936 | 193894 | None | 0 | Human | Binding | EC50 | = | 50.12 | 7.30 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 404.1 | 3 | 1 | 4 | 3.69 | O=C1NCCCc2c1cnn2-c1ccnc(Cc2cc(F)cc(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5274093 | 193901 | None | 0 | Human | Binding | EC50 | = | 25.12 | 7.60 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 404.1 | 3 | 0 | 4 | 3.64 | CN1CCc2c(cnn2-c2cc(Cc3cc(F)cc(C(F)(F)F)c3)ccn2)C1=O | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5277794 | 194058 | None | 0 | Human | Binding | EC50 | = | 2.51 | 8.60 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 386.1 | 4 | 1 | 4 | 3.53 | Cc1nn(-c2ccnc(Cc3cc(F)cc(C(F)F)c3)c2)c2c1C(=O)NCC2 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5278255 | 194081 | None | 0 | Human | Binding | EC50 | = | 39.81 | 7.40 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 424.1 | 3 | 1 | 4 | 3.96 | O=C1NCCc2c1cnn2-c1ccnc(Cc2cc(F)c(Cl)c(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5278598 | 194095 | None | 0 | Human | Binding | EC50 | = | 3.98 | 8.40 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 404.1 | 3 | 1 | 4 | 3.61 | Cc1nn(-c2ccnc(Cc3cc(F)cc(C(F)(F)F)c3)c2)c2c1C(=O)NCC2 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5279049 | 194120 | None | 0 | Human | Binding | IC50 | = | 12000.00 | 4.92 | - | 1 | Inhibition of GPR52 (unknown origin) | ChEMBL | 372.2 | 2 | 0 | 6 | 2.94 | C=C1C(=O)O[C@@H]2C/C=C(\C)CC3C=C(C[C@H](OC(=O)/C(C)=C\C)[C@@H]12)C(=O)O3 | https://dx.doi.org/10.1021/acs.jmedchem.2c00799 | |
| CHEMBL5280513 | 194182 | None | 0 | Human | Binding | EC50 | = | 100.00 | 7.00 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 390.1 | 3 | 1 | 4 | 3.30 | O=C1NCCc2c1cnn2-c1cncc(Cc2cc(F)cc(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5282094 | 194251 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 404.1 | 3 | 1 | 4 | 3.61 | Cc1nn(-c2cncc(Cc3cc(F)cc(C(F)(F)F)c3)c2)c2c1C(=O)NCC2 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5284353 | 194360 | None | 8 | Human | Binding | EC50 | = | 31.62 | 7.50 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 390.1 | 3 | 1 | 4 | 3.30 | O=C1NCCc2c1cnn2-c1ccnc(Cc2cc(F)cc(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5284353 | 194360 | None | 8 | Human | Binding | EC50 | = | 27.50 | 7.56 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 390.1 | 3 | 1 | 4 | 3.30 | O=C1NCCc2c1cnn2-c1ccnc(Cc2cc(F)cc(C(F)(F)F)c2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5284809 | 194374 | None | 0 | Human | Binding | EC50 | = | 25.12 | 7.60 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 371.1 | 3 | 0 | 4 | 4.40 | O=C1CCCc2c1cnn2-c1cc(Cc2cccc(C(F)(F)F)c2)ccn1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
| CHEMBL5287006 | 194478 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 1 | Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis | ChEMBL | 390.1 | 3 | 1 | 4 | 3.30 | O=C1NCCc2c1cnn2-c1cc(Cc2cc(F)cc(C(F)(F)F)c2)ccn1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00052 | |
Showing 1 to 20 of 26 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| CHEMBL2375494 | 89657 | None | 15 | Human | Functional | IC50 | = | 650.00 | 6.19 | 1 | 2 | Antagonist activity at GPR52 (unknown origin) expressed in HEK293 cells assessed as inhibition of WO459-induced cAMP accumulation preincubated for 15 mins followed by WO459 addition and measured after 30 mins by LANCE Ultra cAMP kit based microplate reader analysis | ChEMBL | 236.1 | 5 | 0 | 1 | 4.06 | O=C(/C=C/CCc1ccccc1)c1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c01133 | |
| CHEMBL2375494 | 89657 | None | 15 | Mouse | Functional | IC50 | = | 650.00 | 6.19 | -1 | 2 | In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in mHTT levels | ChEMBL | 236.1 | 5 | 0 | 1 | 4.06 | O=C(/C=C/CCc1ccccc1)c1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c02235 | |
| CHEMBL240484 | 91578 | None | 20 | Human | Functional | IC50 | = | 5450.00 | 5.26 | 1 | 2 | Antagonist activity at GPR52 (unknown origin) expressed in HEK293 cells assessed as inhibition of WO459-induced cAMP accumulation preincubated for 15 mins followed by WO459 addition and measured after 30 mins by LANCE Ultra cAMP kit based microplate reader analysis | ChEMBL | 264.2 | 7 | 0 | 1 | 4.38 | O=C(/C=C/CCc1ccccc1)CCc1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c01133 | |
| CHEMBL240484 | 91578 | None | 20 | Mouse | Functional | IC50 | = | 6000.00 | 5.22 | -1 | 2 | In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in mHTT levels | ChEMBL | 264.2 | 7 | 0 | 1 | 4.38 | O=C(/C=C/CCc1ccccc1)CCc1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c02235 | |
| CHEMBL3297807 | 112479 | None | 0 | Human | Functional | EC50 | = | 208.93 | 6.68 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 441.2 | 6 | 2 | 3 | 4.64 | O=C(NCCO)c1cccc(-c2cccc3c2OC(Cc2cccc(C(F)(F)F)c2)C3)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3297809 | 112480 | None | 0 | Human | Functional | EC50 | = | 81.28 | 7.09 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 453.2 | 6 | 2 | 3 | 5.74 | Cc1c(Cc2cccc(C(F)(F)F)c2)oc2c(-c3cccc(C(=O)NCCO)c3)cccc12 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3297810 | 112481 | None | 0 | Human | Functional | EC50 | = | 54.95 | 7.26 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 468.1 | 6 | 2 | 3 | 5.39 | NC(=O)CNC(=O)c1cccc(-c2cccc3cc(Cc4cccc(C(F)(F)F)c4)sc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3297811 | 112482 | None | 0 | Human | Functional | EC50 | = | 42.66 | 7.37 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 469.1 | 7 | 1 | 3 | 6.55 | COCCNC(=O)c1cccc(-c2cccc3cc(Cc4cccc(C(F)(F)F)c4)sc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3298233 | 112508 | None | 9 | Human | Functional | EC50 | = | 29.51 | 7.53 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 453.1 | 7 | 1 | 3 | 6.33 | COCCNC(=O)c1cccc(-c2cccc3cc(Cc4cc(F)cc(Cl)c4)sc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3298234 | 112509 | None | 0 | Human | Functional | EC50 | = | 83.18 | 7.08 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 486.1 | 6 | 2 | 3 | 5.53 | NC(=O)CNC(=O)c1cccc(-c2ccc(F)c3cc(Cc4cccc(C(F)(F)F)c4)sc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299120 | 112601 | None | 0 | Human | Functional | EC50 | = | 34.67 | 7.46 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 439.1 | 6 | 2 | 3 | 5.43 | O=C(NCCO)c1cccc(-c2cccc3cc(Cc4cccc(C(F)(F)F)c4)oc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299121 | 112602 | None | 0 | Human | Functional | EC50 | = | 38.02 | 7.42 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 455.1 | 6 | 2 | 3 | 5.90 | O=C(NCCO)c1cccc(-c2cccc3sc(Cc4cccc(C(F)(F)F)c4)cc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299122 | 112603 | None | 0 | Human | Functional | EC50 | = | 37.15 | 7.43 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 455.1 | 6 | 2 | 3 | 5.90 | O=C(NCCO)c1cccc(-c2cccc3cc(Cc4cccc(C(F)(F)F)c4)sc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299123 | 112604 | None | 0 | Human | Functional | EC50 | = | 38.90 | 7.41 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 439.2 | 6 | 2 | 4 | 4.49 | O=C(NCCO)c1cccc(-c2cccc3nn(Cc4cccc(C(F)(F)F)c4)cc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299124 | 112605 | None | 0 | Human | Functional | EC50 | = | 64.57 | 7.19 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 439.2 | 6 | 2 | 4 | 4.49 | O=C(NCCO)c1cccc(-c2cccc3cn(Cc4cccc(C(F)(F)F)c4)nc23)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL3299125 | 112606 | None | 0 | Human | Functional | EC50 | = | 645.65 | 6.19 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as cAMP production after 30 mins by Alphascreen assay | ChEMBL | 441.2 | 6 | 2 | 3 | 4.64 | O=C(NCCO)c1cccc(-c2cccc3c2CC(Cc2cccc(C(F)(F)F)c2)O3)c1 | https://dx.doi.org/10.1021/jm5002919 | |
| CHEMBL4059658 | 155889 | None | 0 | Human | Functional | EC50 | = | 11.00 | 7.96 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as increase in cAMP level after 30 mins by AlphaScreen assay | ChEMBL | 408.1 | 4 | 1 | 3 | 5.28 | Cc1cc(-c2sc(Cc3cc(F)cc(C(F)(F)F)c3)nc2C)ccc1C(N)=O | https://dx.doi.org/10.1016/j.bmc.2017.03.064 | |
| CHEMBL4062229 | 156115 | None | 0 | Human | Functional | EC50 | = | 170.00 | 6.77 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as increase in cAMP level after 30 mins by AlphaScreen assay | ChEMBL | 406.1 | 5 | 1 | 4 | 4.84 | COc1cc(-c2sc(Cc3cccc(C(F)(F)F)c3)nc2C)ccc1C(N)=O | https://dx.doi.org/10.1016/j.bmc.2017.03.064 | |
| CHEMBL4064577 | 156313 | None | 0 | Human | Functional | EC50 | = | 210.00 | 6.68 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as increase in cAMP level after 30 mins by AlphaScreen assay | ChEMBL | 356.1 | 4 | 1 | 3 | 4.77 | Cc1cc(-c2sc(Cc3ccc(Cl)cc3)nc2C)ccc1C(N)=O | https://dx.doi.org/10.1016/j.bmc.2017.03.064 | |
| CHEMBL4070849 | 156874 | None | 0 | Human | Functional | EC50 | = | 260.00 | 6.58 | - | 1 | Agonist activity at human GPR52 expressed in CHO cells assessed as increase in cAMP level after 30 mins by AlphaScreen assay | ChEMBL | 340.1 | 4 | 1 | 3 | 4.26 | Cc1cc(-c2sc(Cc3cccc(F)c3)nc2C)ccc1C(N)=O | https://dx.doi.org/10.1016/j.bmc.2017.03.064 | |
Showing 1 to 20 of 322 entries