Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 5803 | 394 | None | 20 | Human | Functional | pEC50 | = | 7 | 7.0 | -2 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 294 | 4 | 1 | 3 | 4.2 | CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C | 10.1016/j.bmc.2018.09.015 | ||
| 854189 | 394 | None | 20 | Human | Functional | pEC50 | = | 7 | 7.0 | -2 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 294 | 4 | 1 | 3 | 4.2 | CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL594671 | 394 | None | 20 | Human | Functional | pEC50 | = | 7 | 7.0 | -2 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 294 | 4 | 1 | 3 | 4.2 | CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C | 10.1016/j.bmc.2018.09.015 | ||
| 46235794 | 163030 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | 2 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 414 | 7 | 1 | 4 | 4.8 | CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4174307 | 163030 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | 2 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 414 | 7 | 1 | 4 | 4.8 | CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| 67209751 | 162263 | None | 0 | Mouse | Functional | pEC50 | = | 7 | 7.0 | -3 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 505 | 10 | 1 | 6 | 6.0 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4162307 | 162263 | None | 0 | Mouse | Functional | pEC50 | = | 7 | 7.0 | -3 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 505 | 10 | 1 | 6 | 6.0 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| 117898644 | 163192 | None | 0 | Mouse | Functional | pEC50 | = | 7 | 7.0 | -3 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 515 | 10 | 1 | 7 | 5.7 | CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4177037 | 163192 | None | 0 | Mouse | Functional | pEC50 | = | 7 | 7.0 | -3 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 515 | 10 | 1 | 7 | 5.7 | CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| 145953626 | 162606 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 423 | 4 | 1 | 3 | 5.3 | O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4167577 | 162606 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 423 | 4 | 1 | 3 | 5.3 | O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145953603 | 162575 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 432 | 4 | 1 | 5 | 4.3 | C#Cc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4167161 | 162575 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 432 | 4 | 1 | 5 | 4.3 | C#Cc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145953670 | 162657 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 424 | 4 | 1 | 4 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4168456 | 162657 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 424 | 4 | 1 | 4 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 162666399 | 182491 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay |
ChEMBL | 468 | 6 | 2 | 4 | 3.8 | CC(Oc1cccc(Cl)c1)C(=O)N(C)[C@H]1CC[C@]2(CC1)NC(=N)N(Cc1ccccc1)C2=O | 10.1016/j.bmcl.2020.127460 | ||
| CHEMBL4785193 | 182491 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay |
ChEMBL | 468 | 6 | 2 | 4 | 3.8 | CC(Oc1cccc(Cl)c1)C(=O)N(C)[C@H]1CC[C@]2(CC1)NC(=N)N(Cc1ccccc1)C2=O | 10.1016/j.bmcl.2020.127460 | ||
| 57520598 | 1812 | None | 33 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/acs.jmedchem.8b00855 | ||
| 8417 | 1812 | None | 33 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL3353541 | 1812 | None | 33 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/acs.jmedchem.8b00855 | ||
| DB15406 | 1812 | None | 33 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/acs.jmedchem.8b00855 | ||
| 145951537 | 162804 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 3 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 537 | 10 | 1 | 7 | 6.0 | COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4170829 | 162804 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 3 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 537 | 10 | 1 | 7 | 6.0 | COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| 53302677 | 162942 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 474 | 8 | 1 | 4 | 5.9 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4172928 | 162942 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1 | 2 | Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 474 | 8 | 1 | 4 | 5.9 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| 67258265 | 162823 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 435 | 5 | 1 | 3 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4171128 | 162823 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 435 | 5 | 1 | 3 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145957026 | 162302 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 453 | 5 | 1 | 4 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2cccc(Cl)c2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4162808 | 162302 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 453 | 5 | 1 | 4 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2cccc(Cl)c2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 117898634 | 162489 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | -5 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 479 | 10 | 1 | 6 | 5.5 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4165748 | 162489 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | -5 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 479 | 10 | 1 | 6 | 5.5 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| 145971768 | 163216 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 448 | 4 | 1 | 4 | 5.2 | N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4177359 | 163216 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 448 | 4 | 1 | 4 | 5.2 | N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145971768 | 163216 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 448 | 4 | 1 | 4 | 5.2 | N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4177359 | 163216 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 448 | 4 | 1 | 4 | 5.2 | N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145954653 | 162733 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 420 | 5 | 1 | 5 | 4.1 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4169673 | 162733 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 420 | 5 | 1 | 5 | 4.1 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 53302677 | 162942 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1 | 2 | Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay |
ChEMBL | 474 | 8 | 1 | 4 | 5.9 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 | 10.1016/j.bmcl.2020.127460 | ||
| CHEMBL4172928 | 162942 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 1 | 2 | Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay |
ChEMBL | 474 | 8 | 1 | 4 | 5.9 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 | 10.1016/j.bmcl.2020.127460 | ||
| 145951076 | 163068 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 408 | 4 | 1 | 5 | 4.3 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4175033 | 163068 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 408 | 4 | 1 | 5 | 4.3 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145954653 | 162733 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 420 | 5 | 1 | 5 | 4.1 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4169673 | 162733 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay |
ChEMBL | 420 | 5 | 1 | 5 | 4.1 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145953670 | 162657 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 424 | 4 | 1 | 4 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4168456 | 162657 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay |
ChEMBL | 424 | 4 | 1 | 4 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 5803 | 394 | None | 20 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | 2 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 294 | 4 | 1 | 3 | 4.2 | CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C | 10.1016/j.bmc.2018.09.015 | ||
| 854189 | 394 | None | 20 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | 2 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 294 | 4 | 1 | 3 | 4.2 | CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL594671 | 394 | None | 20 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | 2 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 294 | 4 | 1 | 3 | 4.2 | CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C | 10.1016/j.bmc.2018.09.015 | ||
| 67210172 | 162553 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -5 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 440 | 8 | 1 | 4 | 5.3 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4166818 | 162553 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -5 | 2 | Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method |
ChEMBL | 440 | 8 | 1 | 4 | 5.3 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
Showing 1 to 50 of 678 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 171356818 | 193981 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay |
ChEMBL | 286 | 4 | 2 | 4 | 2.1 | O=c1cc(CCCCCl)c2c(=O)[nH]c(=S)[nH]c2o1 | 10.1039/d2md00076h | ||
| CHEMBL5275861 | 193981 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay |
ChEMBL | 286 | 4 | 2 | 4 | 2.1 | O=c1cc(CCCCCl)c2c(=O)[nH]c(=S)[nH]c2o1 | 10.1039/d2md00076h | ||
| 137633536 | 156386 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | - | 0 | Agonist activity at human FFA2 receptor by FLIPR assayAgonist activity at human FFA2 receptor by FLIPR assay |
ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | ||
| CHEMBL4065397 | 156386 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | - | 0 | Agonist activity at human FFA2 receptor by FLIPR assayAgonist activity at human FFA2 receptor by FLIPR assay |
ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | ||
| 171346683 | 194381 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay |
ChEMBL | 270 | 4 | 2 | 4 | 0.7 | O=c1[nH]c(=O)c2c(CCCCCl)cc(=O)oc2[nH]1 | 10.1039/d2md00076h | ||
| CHEMBL5284951 | 194381 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay |
ChEMBL | 270 | 4 | 2 | 4 | 0.7 | O=c1[nH]c(=O)c2c(CCCCCl)cc(=O)oc2[nH]1 | 10.1039/d2md00076h | ||
| 171343909 | 193728 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay |
ChEMBL | 252 | 3 | 2 | 4 | 1.9 | CCCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 | 10.1039/d2md00076h | ||
| CHEMBL5270112 | 193728 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay |
ChEMBL | 252 | 3 | 2 | 4 | 1.9 | CCCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 | 10.1039/d2md00076h | ||
| 57520598 | 1812 | None | 33 | Human | Binding | pIC50 | = | 6.3 | 6.3 | - | 0 | Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/jm5012885 | ||
| 8417 | 1812 | None | 33 | Human | Binding | pIC50 | = | 6.3 | 6.3 | - | 0 | Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/jm5012885 | ||
| CHEMBL3353541 | 1812 | None | 33 | Human | Binding | pIC50 | = | 6.3 | 6.3 | - | 0 | Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/jm5012885 | ||
| DB15406 | 1812 | None | 33 | Human | Binding | pIC50 | = | 6.3 | 6.3 | - | 0 | Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry |
ChEMBL | 484 | 8 | 1 | 4 | 5.1 | OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl | 10.1021/jm5012885 | ||
| 145951537 | 162804 | None | 0 | Human | Binding | pKi | = | 7 | 7.0 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 537 | 10 | 1 | 7 | 6.0 | COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4170829 | 162804 | None | 0 | Human | Binding | pKi | = | 7 | 7.0 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 537 | 10 | 1 | 7 | 6.0 | COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| 145957346 | 162064 | None | 0 | Human | Binding | pKi | = | 5.9 | 5.9 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 419 | 5 | 1 | 4 | 4.7 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4159019 | 162064 | None | 0 | Human | Binding | pKi | = | 5.9 | 5.9 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 419 | 5 | 1 | 4 | 4.7 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 67209751 | 162263 | None | 0 | Human | Binding | pKi | = | 6.8 | 6.8 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 505 | 10 | 1 | 6 | 6.0 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4162307 | 162263 | None | 0 | Human | Binding | pKi | = | 6.8 | 6.8 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 505 | 10 | 1 | 6 | 6.0 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| 117898644 | 163192 | None | 0 | Human | Binding | pKi | = | 6.8 | 6.8 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 515 | 10 | 1 | 7 | 5.7 | CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4177037 | 163192 | None | 0 | Human | Binding | pKi | = | 6.8 | 6.8 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 515 | 10 | 1 | 7 | 5.7 | CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| 53302677 | 162942 | None | 1 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 474 | 8 | 1 | 4 | 5.9 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4172928 | 162942 | None | 1 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 474 | 8 | 1 | 4 | 5.9 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| 67209297 | 162893 | None | 0 | Human | Binding | pKi | = | 5.7 | 5.7 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 422 | 7 | 1 | 5 | 4.3 | CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4172349 | 162893 | None | 0 | Human | Binding | pKi | = | 5.7 | 5.7 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 422 | 7 | 1 | 5 | 4.3 | CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| 138319694 | 163169 | None | 33 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 442 | 4 | 1 | 5 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4176503 | 163169 | None | 33 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 442 | 4 | 1 | 5 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 117898634 | 162489 | None | 0 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 479 | 10 | 1 | 6 | 5.5 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4165748 | 162489 | None | 0 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 479 | 10 | 1 | 6 | 5.5 | COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 | 10.1016/j.bmc.2018.09.015 | ||
| 67209218 | 162975 | None | 0 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 406 | 7 | 1 | 4 | 5.1 | CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4173387 | 162975 | None | 0 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 406 | 7 | 1 | 4 | 5.1 | CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| 145951986 | 162799 | None | 0 | Human | Binding | pKi | = | 6.5 | 6.5 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 453 | 5 | 1 | 4 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4170748 | 162799 | None | 0 | Human | Binding | pKi | = | 6.5 | 6.5 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 453 | 5 | 1 | 4 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 145953670 | 162657 | None | 0 | Human | Binding | pKi | = | 6.4 | 6.4 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 424 | 4 | 1 | 4 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4168456 | 162657 | None | 0 | Human | Binding | pKi | = | 6.4 | 6.4 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 424 | 4 | 1 | 4 | 5.0 | Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 67210172 | 162553 | None | 0 | Human | Binding | pKi | = | 6.4 | 6.4 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 440 | 8 | 1 | 4 | 5.3 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4166818 | 162553 | None | 0 | Human | Binding | pKi | = | 6.4 | 6.4 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 440 | 8 | 1 | 4 | 5.3 | O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| 67258265 | 162823 | None | 0 | Human | Binding | pKi | = | 6.3 | 6.3 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 435 | 5 | 1 | 3 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4171128 | 162823 | None | 0 | Human | Binding | pKi | = | 6.3 | 6.3 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 435 | 5 | 1 | 3 | 5.4 | COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 117898651 | 162988 | None | 0 | Human | Binding | pKi | = | 7.2 | 7.2 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 541 | 10 | 1 | 7 | 6.2 | O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4173663 | 162988 | None | 0 | Human | Binding | pKi | = | 7.2 | 7.2 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 541 | 10 | 1 | 7 | 6.2 | O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 | 10.1016/j.bmc.2018.09.015 | ||
| 46235794 | 163030 | None | 0 | Human | Binding | pKi | = | 6.1 | 6.1 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 414 | 7 | 1 | 4 | 4.8 | CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| CHEMBL4174307 | 163030 | None | 0 | Human | Binding | pKi | = | 6.1 | 6.1 | - | 1 | Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method |
ChEMBL | 414 | 7 | 1 | 4 | 4.8 | CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 | 10.1016/j.bmc.2018.09.015 | ||
| 145953626 | 162606 | None | 0 | Human | Binding | pKi | = | 6.0 | 6.0 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 423 | 4 | 1 | 3 | 5.3 | O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| CHEMBL4167577 | 162606 | None | 0 | Human | Binding | pKi | = | 6.0 | 6.0 | - | 1 | Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry |
ChEMBL | 423 | 4 | 1 | 3 | 5.3 | O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/acs.jmedchem.8b00855 | ||
| 10107 | 3883 | None | 0 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Binding affinity for hFFA2.Binding affinity for hFFA2. |
Guide to Pharmacology | 442 | 4 | 1 | 5 | 5.0 | O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C | 30247908 | ||
| 137321147 | 3883 | None | 0 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Binding affinity for hFFA2.Binding affinity for hFFA2. |
Guide to Pharmacology | 442 | 4 | 1 | 5 | 5.0 | O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C | 30247908 | ||
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