Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 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
11954197 166 None 27 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
4350 166 None 27 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
CHEMBL4788348 166 None 27 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
162663790 182004 None 0 Human Functional pEC50 = 10.0 10.0 15 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
CHEMBL4779254 182004 None 0 Human Functional pEC50 = 10.0 10.0 15 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
11954197 166 None 27 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
4350 166 None 27 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
CHEMBL4788348 166 None 27 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
11954197 166 None 27 Mouse Functional pEC50 = 9.2 9.2 -1 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
4350 166 None 27 Mouse Functional pEC50 = 9.2 9.2 -1 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
CHEMBL4788348 166 None 27 Mouse Functional pEC50 = 9.2 9.2 -1 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
440985 182712 None 14 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 6 3 3 5.3 CC(CO)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.bmcl.2016.09.029
CHEMBL4788277 182712 None 14 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 6 3 3 5.3 CC(CO)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.bmcl.2016.09.029
162663790 182004 None 0 Mouse Functional pEC50 = 8.8 8.8 -15 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
CHEMBL4779254 182004 None 0 Mouse Functional pEC50 = 8.8 8.8 -15 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
107722 170 None 32 Human Functional pEC50 = 7.0 7.0 - 1
GPCR PRESTO-Tango dose-response in agonist mode with target: GPR183GPCR PRESTO-Tango dose-response in agonist mode with target: GPR183
ChEMBL 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 10.6019/CHEMBL5442687
4351 170 None 32 Human Functional pEC50 = 7.0 7.0 - 1
GPCR PRESTO-Tango dose-response in agonist mode with target: GPR183GPCR PRESTO-Tango dose-response in agonist mode with target: GPR183
ChEMBL 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 10.6019/CHEMBL5442687
CHEMBL497207 170 None 32 Human Functional pEC50 = 7.0 7.0 - 1
GPCR PRESTO-Tango dose-response in agonist mode with target: GPR183GPCR PRESTO-Tango dose-response in agonist mode with target: GPR183
ChEMBL 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 10.6019/CHEMBL5442687
162656664 180963 None 0 Mouse Functional pEC50 = 7.8 7.8 -3 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
CHEMBL4757291 180963 None 0 Mouse Functional pEC50 = 7.8 7.8 -3 2
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
1599 2341 None 28 Human Functional pEC50 = 5.8 5.8 -912 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
3955 2341 None 28 Human Functional pEC50 = 5.8 5.8 -912 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
3955.0 2341 None 28 Human Functional pEC50 = 5.8 5.8 -912 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
7215 2341 None 28 Human Functional pEC50 = 5.8 5.8 -912 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
CHEMBL841 2341 None 28 Human Functional pEC50 = 5.8 5.8 -912 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
DB00836 2341 None 28 Human Functional pEC50 = 5.8 5.8 -912 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
4355 177 None 13 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
473142 177 None 13 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
CHEMBL3311219 177 None 13 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 10.1016/j.bmcl.2016.09.029
162656664 180963 None 0 Human Functional pEC50 = 8.4 8.4 3 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
CHEMBL4757291 180963 None 0 Human Functional pEC50 = 8.4 8.4 3 2
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 486 5 3 3 6.4 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@@]3(O)C(F)(F)F 10.1016/j.bmcl.2016.09.029
3036864 205211 None 16 Human Functional pEC50 = 5.3 5.3 -12302 13
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.6019/CHEMBL5442687
CHEMBL1256645 205211 None 16 Human Functional pEC50 = 5.3 5.3 -12302 13
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.6019/CHEMBL5442687
CHEMBL1814790 205211 None 16 Human Functional pEC50 = 5.3 5.3 -12302 13
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.6019/CHEMBL5442687
CHEMBL62 205211 None 16 Human Functional pEC50 = 5.3 5.3 -12302 13
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.6019/CHEMBL5442687
67426622 181816 None 2 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 6 3 3 5.3 CC(CO)CCC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@@H]3O 10.1016/j.bmcl.2016.09.029
CHEMBL4776911 181816 None 2 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysisAgonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
ChEMBL 418 6 3 3 5.3 CC(CO)CCC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@H](O)CC1=C[C@@H]3O 10.1016/j.bmcl.2016.09.029
73330414 120997 None 0 Human Functional pIC50 = 9.4 9.4 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 432 3 0 2 4.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL3560809 120997 None 0 Human Functional pIC50 = 9.4 9.4 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 432 3 0 2 4.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc(Cl)cc2)CC1 nan
13052 2820 None 48 Human Functional pIC50 = 9.3 9.3 3 2
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br nan
36295259 2820 None 48 Human Functional pIC50 = 9.3 9.3 3 2
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br nan
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 9.3 9.3 3 2
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br nan
73330413 120999 None 0 Human Functional pIC50 = 9.2 9.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 398 3 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccccc2)CC1 nan
CHEMBL3560864 120999 None 0 Human Functional pIC50 = 9.2 9.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 398 3 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccccc2)CC1 nan
39566276 121001 None 0 Human Functional pIC50 = 9.0 9.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 412 3 0 2 3.8 Cc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3560888 121001 None 0 Human Functional pIC50 = 9.0 9.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 412 3 0 2 3.8 Cc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
73169083 120974 None 29 Human Functional pIC50 = 9.0 9.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 418 4 0 2 4.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
CHEMBL3560331 120974 None 29 Human Functional pIC50 = 9.0 9.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 418 4 0 2 4.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
13052 2820 None 48 Human Functional pIC50 = 9.0 9.0 3 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.6019/CHEMBL5442687
36295259 2820 None 48 Human Functional pIC50 = 9.0 9.0 3 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.6019/CHEMBL5442687
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 9.0 9.0 3 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.6019/CHEMBL5442687
71295857 120969 None 0 Human Functional pIC50 = 8.9 8.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 426 4 0 3 3.3 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)C2=Cc3ccccc3CC2)CC1 nan
CHEMBL3560117 120969 None 0 Human Functional pIC50 = 8.9 8.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 426 4 0 3 3.3 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)C2=Cc3ccccc3CC2)CC1 nan
73330415 121016 None 0 Human Functional pIC50 = 8.9 8.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 422 3 0 2 4.6 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL3561364 121016 None 0 Human Functional pIC50 = 8.9 8.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 422 3 0 2 4.6 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)c2ccc(Cl)cc2)CC1 nan
73330396 121030 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 416 4 0 2 4.3 Cc1cc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)ccc1F nan
CHEMBL3561756 121030 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 416 4 0 2 4.3 Cc1cc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)ccc1F nan
71295907 121018 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 512 4 0 3 3.8 O=C(/C=C/c1ccc(Br)cc1)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3561399 121018 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 512 4 0 3 3.8 O=C(/C=C/c1ccc(Br)cc1)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
73330421 120967 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 2 5.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3560041 120967 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 2 5.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 nan
73330424 120981 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 423 3 0 3 3.3 N#Cc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3560453 120981 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 423 3 0 3 3.3 N#Cc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
73330403 121013 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 398 4 0 2 4.1 Cc1ccc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3561255 121013 None 0 Human Functional pIC50 = 8.8 8.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 398 4 0 2 4.1 Cc1ccc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
46399493 120992 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 466 3 0 2 4.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL3560732 120992 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 466 3 0 2 4.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1 nan
13052 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
86580332 111107 None 1 Mouse Functional pIC50 = 7 7.0 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 416 5 0 3 2.7 O=C(COc1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262877 111107 None 1 Mouse Functional pIC50 = 7 7.0 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 416 5 0 3 2.7 O=C(COc1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
172462349 196759 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 440 3 1 5 2.9 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc3[nH]ccc3c2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5431534 196759 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 440 3 1 5 2.9 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc3[nH]ccc3c2)CC1 10.1021/acs.jmedchem.3c01364
172465299 196927 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 416 3 0 6 2.1 Cc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5435007 196927 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 416 3 0 6 2.1 Cc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
13052 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
26204807 120996 None 1 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc(Cl)c2)CC1 nan
CHEMBL3560763 120996 None 1 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc(Cl)c2)CC1 nan
172466517 196719 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 440 4 0 4 3.4 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)C2(c3ccccc3)CC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5430675 196719 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 440 4 0 4 3.4 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)C2(c3ccccc3)CC2)CC1 10.1021/acs.jmedchem.3c01364
8381950 120961 None 0 Human Functional pIC50 = 7.0 7.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 6 0 3 2.9 O=C(CCc1ccc(F)cc1)N1CCN(S(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3559877 120961 None 0 Human Functional pIC50 = 7.0 7.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 6 0 3 2.9 O=C(CCc1ccc(F)cc1)N1CCN(S(=O)(=O)/C=C/c2ccccc2)CC1 nan
2671117 120983 None 1 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 404 5 0 4 2.4 COc1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
CHEMBL3560467 120983 None 1 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 404 5 0 4 2.4 COc1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
71295891 120977 None 0 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 430 4 0 3 3.7 CC(C)(C)c1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
CHEMBL3560404 120977 None 0 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 430 4 0 3 3.7 CC(C)(C)c1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
2634553 120958 None 2 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 374 4 0 3 2.4 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccccc2)CC1 nan
CHEMBL3559792 120958 None 2 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 374 4 0 3 2.4 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccccc2)CC1 nan
86579984 111123 None 0 Human Functional pIC50 = 7.9 7.9 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262892 111123 None 0 Human Functional pIC50 = 7.9 7.9 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
26867780 120980 None 0 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 419 5 0 5 2.3 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL3560431 120980 None 0 Human Functional pIC50 = 7.9 7.9 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 419 5 0 5 2.3 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc([N+](=O)[O-])cc2)CC1 nan
171781219 196498 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 441 4 0 4 2.9 COc1ccc(C(=O)N2CC3(CN(C(=O)/C=C/c4ccc(Br)cc4)C3)C2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5425366 196498 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 441 4 0 4 2.9 COc1ccc(C(=O)N2CC3(CN(C(=O)/C=C/c4ccc(Br)cc4)C3)C2)cn1 10.1021/acs.jmedchem.3c01364
1072081 111106 None 14 Human Functional pIC50 = 6.9 6.9 6 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Functional pIC50 = 6.9 6.9 6 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
172460662 196516 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 457 4 0 7 2.0 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(N3CCC3)nc2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5425720 196516 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 457 4 0 7 2.0 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(N3CCC3)nc2)CC1 10.1021/acs.jmedchem.3c01364
86579984 111123 None 0 Human Functional pIC50 = 7.9 7.9 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262892 111123 None 0 Human Functional pIC50 = 7.9 7.9 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
13052 2820 None 48 Mouse Functional pIC50 = 7.9 7.9 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Mouse Functional pIC50 = 7.9 7.9 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Mouse Functional pIC50 = 7.9 7.9 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
91754 85284 None 43 Human Functional pIC50 = 7.9 7.9 -2 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 364 3 0 4 5.2 CC(C)(C)c1ccc(CSc2cnn(C(C)(C)C)c(=O)c2Cl)cc1 10.6019/CHEMBL5442687
CHEMBL225963 85284 None 43 Human Functional pIC50 = 7.9 7.9 -2 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 364 3 0 4 5.2 CC(C)(C)c1ccc(CSc2cnn(C(C)(C)C)c(=O)c2Cl)cc1 10.6019/CHEMBL5442687
172448012 195926 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 431 4 0 6 2.4 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)nc1 10.1021/acs.jmedchem.3c01364
CHEMBL5413510 195926 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 431 4 0 6 2.4 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)nc1 10.1021/acs.jmedchem.3c01364
172457410 196376 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 502 5 0 8 2.4 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(OC3CCOCC3)nc2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5422521 196376 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 502 5 0 8 2.4 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(OC3CCOCC3)nc2)CC1 10.1021/acs.jmedchem.3c01364
73330394 120960 None 0 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 2 5.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
CHEMBL3559855 120960 None 0 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 2 5.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
26867530 121019 None 0 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 478 6 0 4 3.4 CCOc1ccc(/C=C/C(=O)N2CCN(S(=O)(=O)c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3561444 121019 None 0 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 478 6 0 4 3.4 CCOc1ccc(/C=C/C(=O)N2CCN(S(=O)(=O)c3ccc(Br)cc3)CC2)cc1 nan
13052 2820 None 48 Mouse Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Mouse Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Mouse Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
898463 120991 None 5 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 322 3 0 2 2.6 CCN1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
CHEMBL3560691 120991 None 5 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 322 3 0 2 2.6 CCN1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
90655991 111125 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262894 111125 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
172447181 195022 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 486 5 0 7 3.1 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(OC3CCCC3)nc2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5395113 195022 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 486 5 0 7 3.1 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(OC3CCCC3)nc2)CC1 10.1021/acs.jmedchem.3c01364
168228703 195329 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 438 3 0 3 4.2 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3occc3c2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5401247 195329 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 438 3 0 3 4.2 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3occc3c2)CC1 10.1021/acs.jmedchem.3c01364
90655991 111125 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262894 111125 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
86579939 111113 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
CHEMBL3262883 111113 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
86579982 111121 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262890 111121 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
86579939 111113 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
CHEMBL3262883 111113 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
86579982 111121 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262890 111121 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
26559312 120994 None 1 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc(Br)c2)CC1 nan
CHEMBL3560750 120994 None 1 Human Functional pIC50 = 7.8 7.8 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc(Br)c2)CC1 nan
90655990 111122 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
CHEMBL3262891 111122 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
86579982 111121 None 0 Mouse Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262890 111121 None 0 Mouse Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
90655990 111122 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
CHEMBL3262891 111122 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
86579982 111121 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262890 111121 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 408 5 0 5 2.5 COC(=O)c1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
2664154 121005 None 2 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 4 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc(F)cc2)CC1 nan
CHEMBL3560941 121005 None 2 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 4 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc(F)cc2)CC1 nan
73330411 121025 None 0 Human Functional pIC50 = 6.7 6.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 3 3.0 O=C(/C=C/c1ccc(Cl)cc1F)N1CCN(S(=O)(=O)c2ccccc2)CC1 nan
CHEMBL3561595 121025 None 0 Human Functional pIC50 = 6.7 6.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 3 3.0 O=C(/C=C/c1ccc(Cl)cc1F)N1CCN(S(=O)(=O)c2ccccc2)CC1 nan
1692 2154 None 25 Human Functional pIC50 = 5.7 5.7 -61 18
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.6019/CHEMBL5442687
5311340 2154 None 25 Human Functional pIC50 = 5.7 5.7 -61 18
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.6019/CHEMBL5442687
CHEMBL140979 2154 None 25 Human Functional pIC50 = 5.7 5.7 -61 18
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.6019/CHEMBL5442687
73330425 120964 None 0 Human Functional pIC50 = 6.7 6.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 448 4 0 3 3.3 Cc1ccccc1/C=C/C(=O)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3559978 120964 None 0 Human Functional pIC50 = 6.7 6.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 448 4 0 3 3.3 Cc1ccccc1/C=C/C(=O)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
86579902 111110 None 1 Human Functional pIC50 = 7.7 7.7 4 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262880 111110 None 1 Human Functional pIC50 = 7.7 7.7 4 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579981 111119 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262889 111119 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
86579902 111110 None 1 Human Functional pIC50 = 7.7 7.7 4 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262880 111110 None 1 Human Functional pIC50 = 7.7 7.7 4 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579981 111119 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262889 111119 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
7750538 120959 None 1 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 4 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccccc2F)CC1 nan
CHEMBL3559845 120959 None 1 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 4 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccccc2F)CC1 nan
2678641 121024 None 1 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 4 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc(F)c2)CC1 nan
CHEMBL3561498 121024 None 1 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 4 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc(F)c2)CC1 nan
86579981 111119 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262889 111119 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
1072081 111106 None 14 Human Functional pIC50 = 6.7 6.7 6 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Functional pIC50 = 6.7 6.7 6 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
24901704 95043 None 55 Human Functional pIC50 = 5.7 5.7 1 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 517 6 2 7 5.7 Cn1cnc(-c2cc3nccc(Oc4ccc(NC(=S)NC(=O)Cc5ccccc5)cc4F)c3s2)c1 10.6019/CHEMBL5442687
CHEMBL254760 95043 None 55 Human Functional pIC50 = 5.7 5.7 1 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 517 6 2 7 5.7 Cn1cnc(-c2cc3nccc(Oc4ccc(NC(=S)NC(=O)Cc5ccccc5)cc4F)c3s2)c1 10.6019/CHEMBL5442687
73330409 120982 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 350 5 0 2 3.4 CCCCN1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
CHEMBL3560464 120982 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 350 5 0 2 3.4 CCCCN1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
73330398 120987 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 420 4 0 2 4.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2cc(F)cc(F)c2)CC1 nan
CHEMBL3560573 120987 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 420 4 0 2 4.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2cc(F)cc(F)c2)CC1 nan
73330410 121031 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 350 4 0 2 3.4 CCC(C)N1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
CHEMBL3561798 121031 None 0 Human Functional pIC50 = 8.7 8.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 350 4 0 2 3.4 CCC(C)N1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
73330406 121004 None 0 Human Functional pIC50 = 8.6 8.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2cccc(F)c2)CC1 nan
CHEMBL3560897 121004 None 0 Human Functional pIC50 = 8.6 8.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2cccc(F)c2)CC1 nan
1220338 59304 None 4 Human Functional pIC50 = 8.6 8.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 384 4 0 2 3.8 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccccc2)CC1 nan
CHEMBL1704801 59304 None 4 Human Functional pIC50 = 8.6 8.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 384 4 0 2 3.8 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccccc2)CC1 nan
86579981 111119 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262889 111119 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 393 5 0 4 2.8 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)cc1 10.1021/jm4019355
170157359 196333 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 431 4 0 6 2.4 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5421607 196333 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 431 4 0 6 2.4 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
86579900 111109 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262879 111109 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86579984 111123 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262892 111123 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
172454177 195870 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 408 4 0 5 2.0 CC(C(=O)N1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1)C1COC1 10.1021/acs.jmedchem.3c01364
CHEMBL5412345 195870 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 408 4 0 5 2.0 CC(C(=O)N1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1)C1COC1 10.1021/acs.jmedchem.3c01364
1072081 111106 None 14 Mouse Functional pIC50 = 6.7 6.7 -6 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Mouse Functional pIC50 = 6.7 6.7 -6 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
172459004 196424 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 487 4 1 8 1.4 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(N3CC[C@H](O)C3)nc2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5423746 196424 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 487 4 1 8 1.4 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(N3CC[C@H](O)C3)nc2)CC1 10.1021/acs.jmedchem.3c01364
86579937 111111 None 1 Mouse Functional pIC50 = 6.7 6.7 -7 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262881 111111 None 1 Mouse Functional pIC50 = 6.7 6.7 -7 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579937 111111 None 1 Mouse Functional pIC50 = 6.7 6.7 -7 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262881 111111 None 1 Mouse Functional pIC50 = 6.7 6.7 -7 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579900 111109 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262879 111109 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86579984 111123 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262892 111123 None 0 Mouse Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 398 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Cl)c(C)c3)CC2)cc1 10.1021/jm4019355
2673966 120988 None 2 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 424 4 0 3 3.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc3ccccc3c2)CC1 nan
CHEMBL3560607 120988 None 2 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 424 4 0 3 3.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc3ccccc3c2)CC1 nan
5721584 121364 None 4 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 324 4 0 2 3.2 O=C(/C=C/c1ccccc1)N1CCN(Cc2ccc(F)cc2)CC1 nan
CHEMBL3561640 121364 None 4 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 324 4 0 2 3.2 O=C(/C=C/c1ccccc1)N1CCN(Cc2ccc(F)cc2)CC1 nan
CHEMBL3580443 121364 None 4 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 324 4 0 2 3.2 O=C(/C=C/c1ccccc1)N1CCN(Cc2ccc(F)cc2)CC1 nan
26204394 121026 None 1 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 442 4 0 3 3.7 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)ccc2Cl)CC1 nan
CHEMBL3561698 121026 None 1 Human Functional pIC50 = 7.7 7.7 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 442 4 0 3 3.7 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)ccc2Cl)CC1 nan
170271557 195010 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 438 3 1 3 3.3 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3[nH]cnc3c2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5394888 195010 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 438 3 1 3 3.3 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3[nH]cnc3c2)CC1 10.1021/acs.jmedchem.3c01364
172457555 196459 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 440 3 1 5 2.9 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5424378 196459 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 440 3 1 5 2.9 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/acs.jmedchem.3c01364
90655991 111125 None 0 Mouse Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262894 111125 None 0 Mouse Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
170157417 195391 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 431 5 0 4 2.8 COc1ccc(C(=O)N2CCN(C(=O)CCc3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5402708 195391 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 431 5 0 4 2.8 COc1ccc(C(=O)N2CCN(C(=O)CCc3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
172457896 196415 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 408 4 0 5 2.1 COC1CC(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)C1 10.1021/acs.jmedchem.3c01364
CHEMBL5423491 196415 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 408 4 0 5 2.1 COC1CC(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)C1 10.1021/acs.jmedchem.3c01364
90655991 111125 None 0 Mouse Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262894 111125 None 0 Mouse Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 396 3 0 3 3.3 O=C(/C=C/c1ccc(Cl)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
86579938 111112 None 1 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262882 111112 None 1 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
172451819 196058 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 432 4 0 7 1.8 COc1cnc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5416074 196058 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 432 4 0 7 1.8 COc1cnc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
86579938 111112 None 1 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262882 111112 None 1 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
71295875 121033 None 0 Human Functional pIC50 = 7.6 7.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 416 6 0 3 3.3 CCCc1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
CHEMBL3561833 121033 None 0 Human Functional pIC50 = 7.6 7.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 416 6 0 3 3.3 CCCc1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
2677523 121000 None 0 Human Functional pIC50 = 7.6 7.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 416 5 0 3 3.5 CC(C)c1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
CHEMBL3560877 121000 None 0 Human Functional pIC50 = 7.6 7.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 416 5 0 3 3.5 CC(C)c1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
1014 1706 None 18 Human Functional pIC50 = 5.6 5.6 -79 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 411 2 1 4 5.2 CC(=O)c1ccc2c(c1)[C@@H]1C=CC[C@@H]1[C@@H](N2)c1cc2OCOc2cc1Br 10.6019/CHEMBL5442687
5322399 1706 None 18 Human Functional pIC50 = 5.6 5.6 -79 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 411 2 1 4 5.2 CC(=O)c1ccc2c(c1)[C@@H]1C=CC[C@@H]1[C@@H](N2)c1cc2OCOc2cc1Br 10.6019/CHEMBL5442687
CHEMBL569766 1706 None 18 Human Functional pIC50 = 5.6 5.6 -79 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 411 2 1 4 5.2 CC(=O)c1ccc2c(c1)[C@@H]1C=CC[C@@H]1[C@@H](N2)c1cc2OCOc2cc1Br 10.6019/CHEMBL5442687
172450379 195603 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 379 2 0 4 2.0 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)N2CCC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5406913 195603 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 379 2 0 4 2.0 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)N2CCC2)CC1 10.1021/acs.jmedchem.3c01364
24996872 107593 None 51 Human Functional pIC50 = 5.6 5.6 -37 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 456 7 0 8 4.0 CC(C)c1noc(N2CCC(COc3ccc(-c4ccc(S(C)(=O)=O)cc4)nc3)CC2)n1 10.6019/CHEMBL5442687
CHEMBL3187503 107593 None 51 Human Functional pIC50 = 5.6 5.6 -37 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 456 7 0 8 4.0 CC(C)c1noc(N2CCC(COc3ccc(-c4ccc(S(C)(=O)=O)cc4)nc3)CC2)n1 10.6019/CHEMBL5442687
26867513 121008 None 0 Human Functional pIC50 = 6.6 6.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccccc1F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3561130 121008 None 0 Human Functional pIC50 = 6.6 6.6 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccccc1F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
172454276 196015 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 409 2 0 5 1.6 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)N2CCOCC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5415152 196015 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 409 2 0 5 1.6 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)N2CCOCC2)CC1 10.1021/acs.jmedchem.3c01364
52936725 61270 None 22 Human Functional pIC50 = 5.6 5.6 -549 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.6019/CHEMBL5442687
CHEMBL1766103 61270 None 22 Human Functional pIC50 = 5.6 5.6 -549 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 432 6 2 4 6.3 Cc1cc(C)cc(-c2cnc3cc(Cl)c(-c4cccc(O)c4)cc3c2OCCCN)c1 10.6019/CHEMBL5442687
86580332 111107 None 1 Human Functional pIC50 = 7.6 7.6 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 416 5 0 3 2.7 O=C(COc1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262877 111107 None 1 Human Functional pIC50 = 7.6 7.6 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 416 5 0 3 2.7 O=C(COc1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86580332 111107 None 1 Human Functional pIC50 = 7.6 7.6 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 416 5 0 3 2.7 O=C(COc1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262877 111107 None 1 Human Functional pIC50 = 7.6 7.6 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 416 5 0 3 2.7 O=C(COc1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
9299233 120968 None 3 Human Functional pIC50 = 7.5 7.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 388 5 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)Cc2ccccc2)CC1 nan
CHEMBL3560082 120968 None 3 Human Functional pIC50 = 7.5 7.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 388 5 0 3 2.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)Cc2ccccc2)CC1 nan
73330412 120970 None 0 Human Functional pIC50 = 7.5 7.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 442 4 2 4 1.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2cccc(B(O)O)c2)CC1 nan
CHEMBL3560195 120970 None 0 Human Functional pIC50 = 7.5 7.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 442 4 2 4 1.1 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2cccc(B(O)O)c2)CC1 nan
73330416 120973 None 0 Human Functional pIC50 = 7.5 7.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccccc2F)CC1 nan
CHEMBL3560274 120973 None 0 Human Functional pIC50 = 7.5 7.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccccc2F)CC1 nan
86579937 111111 None 1 Human Functional pIC50 = 7.5 7.5 7 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262881 111111 None 1 Human Functional pIC50 = 7.5 7.5 7 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579900 111109 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262879 111109 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
90655990 111122 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
CHEMBL3262891 111122 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
86579937 111111 None 1 Human Functional pIC50 = 7.5 7.5 7 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262881 111111 None 1 Human Functional pIC50 = 7.5 7.5 7 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 5 0 3 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579900 111109 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262879 111109 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 412 4 0 2 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
90655990 111122 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
CHEMBL3262891 111122 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 392 4 0 4 2.6 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc4c(c3)CCO4)CC2)cc1 10.1021/jm4019355
170157151 195222 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 430 4 0 5 2.2 COc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5399120 195222 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 430 4 0 5 2.2 COc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
86579940 111114 None 0 Human Functional pIC50 = 7.5 7.5 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262884 111114 None 0 Human Functional pIC50 = 7.5 7.5 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
86579897 111108 None 0 Human Functional pIC50 = 5.5 5.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
CHEMBL3262878 111108 None 0 Human Functional pIC50 = 5.5 5.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
86579897 111108 None 0 Human Functional pIC50 = 5.5 5.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
CHEMBL3262878 111108 None 0 Human Functional pIC50 = 5.5 5.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
71295884 120998 None 0 Human Functional pIC50 = 8.5 8.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 6 0 3 2.6 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)CCc2ccccc2)CC1 nan
CHEMBL3560820 120998 None 0 Human Functional pIC50 = 8.5 8.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 402 6 0 3 2.6 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)CCc2ccccc2)CC1 nan
26867573 121034 None 0 Human Functional pIC50 = 8.5 8.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3561859 121034 None 0 Human Functional pIC50 = 8.5 8.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
2674674 51251 None 4 Human Functional pIC50 = 8.5 8.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 400 5 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL1580410 51251 None 4 Human Functional pIC50 = 8.5 8.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 400 5 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)/C=C/c2ccccc2)CC1 nan
73330404 120979 None 0 Human Functional pIC50 = 8.4 8.4 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 444 6 0 4 3.8 COc1cc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc(OC)c1 nan
CHEMBL3560415 120979 None 0 Human Functional pIC50 = 8.4 8.4 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 444 6 0 4 3.8 COc1cc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc(OC)c1 nan
170157371 195061 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 429 4 0 4 2.9 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5395781 195061 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 429 4 0 4 2.9 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
10348 584 None 43 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 453 7 0 5 5.4 N#Cc1c(cccc1C(F)(F)F)Oc1cccc(c1)OS(=O)(=O)CCCC(F)(F)F 10.6019/CHEMBL5442687
10479060 584 None 43 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 453 7 0 5 5.4 N#Cc1c(cccc1C(F)(F)F)Oc1cccc(c1)OS(=O)(=O)CCCC(F)(F)F 10.6019/CHEMBL5442687
CHEMBL1354658 584 None 43 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 453 7 0 5 5.4 N#Cc1c(cccc1C(F)(F)F)Oc1cccc(c1)OS(=O)(=O)CCCC(F)(F)F 10.6019/CHEMBL5442687
1072066 20311 None 13 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL1305842 20311 None 13 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86579940 111114 None 0 Human Functional pIC50 = 7.5 7.5 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262884 111114 None 0 Human Functional pIC50 = 7.5 7.5 2 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
13050 1071 None 6 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 432 4 0 7 1.8 FC1(OC2=C(O1)C=CC(=C2)/C=C/C(N3CCN(C(C4=CN=C(OC)N=C4)=O)CC3)=O)F 10.1021/acs.jmedchem.3c01364
169494480 1071 None 6 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 432 4 0 7 1.8 FC1(OC2=C(O1)C=CC(=C2)/C=C/C(N3CCN(C(C4=CN=C(OC)N=C4)=O)CC3)=O)F 10.1021/acs.jmedchem.3c01364
CHEMBL5394700 1071 None 6 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 432 4 0 7 1.8 FC1(OC2=C(O1)C=CC(=C2)/C=C/C(N3CCN(C(C4=CN=C(OC)N=C4)=O)CC3)=O)F 10.1021/acs.jmedchem.3c01364
73330408 121036 None 0 Human Functional pIC50 = 6.5 6.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 502 4 0 3 4.0 O=C(/C=C/c1ccccc1C(F)(F)F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3561867 121036 None 0 Human Functional pIC50 = 6.5 6.5 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 502 4 0 3 4.0 O=C(/C=C/c1ccccc1C(F)(F)F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
24775005 3639 None 54 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 485 5 1 5 5.8 C[C@@H]1O[C@H](C)CN(C1)c1ccc(cn1)NC(=O)c1cccc(c1C)c1ccc(cc1)OC(F)(F)F 10.6019/CHEMBL5442687
24775005.0 3639 None 54 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 485 5 1 5 5.8 C[C@@H]1O[C@H](C)CN(C1)c1ccc(cn1)NC(=O)c1cccc(c1C)c1ccc(cc1)OC(F)(F)F 10.6019/CHEMBL5442687
5008 3639 None 54 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 485 5 1 5 5.8 C[C@@H]1O[C@H](C)CN(C1)c1ccc(cn1)NC(=O)c1cccc(c1C)c1ccc(cc1)OC(F)(F)F 10.6019/CHEMBL5442687
8199 3639 None 54 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 485 5 1 5 5.8 C[C@@H]1O[C@H](C)CN(C1)c1ccc(cn1)NC(=O)c1cccc(c1C)c1ccc(cc1)OC(F)(F)F 10.6019/CHEMBL5442687
CHEMBL2105737 3639 None 54 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 485 5 1 5 5.8 C[C@@H]1O[C@H](C)CN(C1)c1ccc(cn1)NC(=O)c1cccc(c1C)c1ccc(cc1)OC(F)(F)F 10.6019/CHEMBL5442687
DB09143 3639 None 54 Human Functional pIC50 = 5.5 5.5 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 485 5 1 5 5.8 C[C@@H]1O[C@H](C)CN(C1)c1ccc(cn1)NC(=O)c1cccc(c1C)c1ccc(cc1)OC(F)(F)F 10.6019/CHEMBL5442687
6603703 208 None 8 Human Functional pIC50 = 5.5 5.5 -1047 18
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.6019/CHEMBL5442687
9637 208 None 8 Human Functional pIC50 = 5.5 5.5 -1047 18
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.6019/CHEMBL5442687
CHEMBL291143 208 None 8 Human Functional pIC50 = 5.5 5.5 -1047 18
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.6019/CHEMBL5442687
36294314 111118 None 1 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262888 111118 None 1 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
36294314 111118 None 1 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262888 111118 None 1 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
487 3634 None 20 Human Functional pIC50 = 5.5 5.5 -1 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442687
60602 3634 None 20 Human Functional pIC50 = 5.5 5.5 -1 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442687
CHEMBL405355 3634 None 20 Human Functional pIC50 = 5.5 5.5 -1 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442687
DB09239 3634 None 20 Human Functional pIC50 = 5.5 5.5 -1 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.6019/CHEMBL5442687
172442400 195508 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 380 3 0 5 2.5 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)OC2CC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5405057 195508 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 380 3 0 5 2.5 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)OC2CC2)CC1 10.1021/acs.jmedchem.3c01364
1072066 20311 None 13 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL1305842 20311 None 13 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
9893924 4750 None 24 Human Functional pIC50 = 5.5 5.5 -117 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442687
CHEMBL103769 4750 None 24 Human Functional pIC50 = 5.5 5.5 -117 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442687
9893924 4750 None 24 Human Functional pIC50 = 5.5 5.5 -117 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442687
CHEMBL103769 4750 None 24 Human Functional pIC50 = 5.5 5.5 -117 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442687
5311122 4068 None 4 Human Functional pIC50 = 5.5 5.5 -295 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 456 7 0 3 6.5 COc1ccc2c(c1)C(CCC2)C(=O)N(c1ccc(cc1)C(C)C)Cc1ccc(cc1)N(C)C 10.6019/CHEMBL5442687
581 4068 None 4 Human Functional pIC50 = 5.5 5.5 -295 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 456 7 0 3 6.5 COc1ccc2c(c1)C(CCC2)C(=O)N(c1ccc(cc1)C(C)C)Cc1ccc(cc1)N(C)C 10.6019/CHEMBL5442687
CHEMBL1628668 4068 None 4 Human Functional pIC50 = 5.5 5.5 -295 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 456 7 0 3 6.5 COc1ccc2c(c1)C(CCC2)C(=O)N(c1ccc(cc1)C(C)C)Cc1ccc(cc1)N(C)C 10.6019/CHEMBL5442687
172439099 195317 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 380 3 0 5 1.3 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)C2COC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5400812 195317 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 380 3 0 5 1.3 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)C2COC2)CC1 10.1021/acs.jmedchem.3c01364
22475020 96056 None 19 Human Functional pIC50 = 5.5 5.5 -323 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.6019/CHEMBL5442687
CHEMBL259656 96056 None 19 Human Functional pIC50 = 5.5 5.5 -323 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.6019/CHEMBL5442687
11978813 721 None 58 Human Functional pIC50 = 5.4 5.4 -363 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442687
11978813.0 721 None 58 Human Functional pIC50 = 5.4 5.4 -363 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442687
5014 721 None 58 Human Functional pIC50 = 5.4 5.4 -363 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442687
7672 721 None 58 Human Functional pIC50 = 5.4 5.4 -363 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442687
CHEMBL2105760 721 None 58 Human Functional pIC50 = 5.4 5.4 -363 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442687
DB09128 721 None 58 Human Functional pIC50 = 5.4 5.4 -363 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.6019/CHEMBL5442687
4534 192011 None 61 Human Functional pIC50 = 5.4 5.4 -42 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 302 5 4 4 3.6 CC(Cc1ccc(O)c(O)c1)C(C)Cc1ccc(O)c(O)c1 10.6019/CHEMBL5442687
CHEMBL52 192011 None 61 Human Functional pIC50 = 5.4 5.4 -42 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 302 5 4 4 3.6 CC(Cc1ccc(O)c(O)c1)C(C)Cc1ccc(O)c(O)c1 10.6019/CHEMBL5442687
156419 938 None 48 Human Functional pIC50 = 5.4 5.4 -85 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442687
156419.0 938 None 48 Human Functional pIC50 = 5.4 5.4 -85 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442687
3308 938 None 48 Human Functional pIC50 = 5.4 5.4 -85 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442687
647 938 None 48 Human Functional pIC50 = 5.4 5.4 -85 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442687
CHEMBL1201284 938 None 48 Human Functional pIC50 = 5.4 5.4 -85 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442687
DB01012 938 None 48 Human Functional pIC50 = 5.4 5.4 -85 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.6019/CHEMBL5442687
56593349 2571 None 25 Human Functional pIC50 = 5.4 5.4 -32 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 506 7 2 5 5.3 CC(Oc1ccccc1C(=O)Nc1ccccc1C(=O)Nc1cccc(c1)S(=O)(=O)C(F)(F)F)C 10.6019/CHEMBL5442687
8322 2571 None 25 Human Functional pIC50 = 5.4 5.4 -32 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 506 7 2 5 5.3 CC(Oc1ccccc1C(=O)Nc1ccccc1C(=O)Nc1cccc(c1)S(=O)(=O)C(F)(F)F)C 10.6019/CHEMBL5442687
CHEMBL3716980 2571 None 25 Human Functional pIC50 = 5.4 5.4 -32 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 506 7 2 5 5.3 CC(Oc1ccccc1C(=O)Nc1ccccc1C(=O)Nc1cccc(c1)S(=O)(=O)C(F)(F)F)C 10.6019/CHEMBL5442687
4223 3992 None 57 Human Functional pIC50 = 5.4 5.4 -16218 17
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442687
6918314 3992 None 57 Human Functional pIC50 = 5.4 5.4 -16218 17
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442687
6918314.0 3992 None 57 Human Functional pIC50 = 5.4 5.4 -16218 17
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442687
7427 3992 None 57 Human Functional pIC50 = 5.4 5.4 -16218 17
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442687
CHEMBL439849 3992 None 57 Human Functional pIC50 = 5.4 5.4 -16218 17
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442687
DB06684 3992 None 57 Human Functional pIC50 = 5.4 5.4 -16218 17
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442687
42642645 16406 None 50 Human Functional pIC50 = 5.4 5.4 -1 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 632 12 2 8 5.8 COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCN1CCOCC1 10.6019/CHEMBL5442687
CHEMBL1230609 16406 None 50 Human Functional pIC50 = 5.4 5.4 -1 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 632 12 2 8 5.8 COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCN1CCOCC1 10.6019/CHEMBL5442687
1179 961 None 28 Human Functional pIC50 = 5.4 5.4 -30 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.6019/CHEMBL5442687
9957278 961 None 28 Human Functional pIC50 = 5.4 5.4 -30 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.6019/CHEMBL5442687
CHEMBL494803 961 None 28 Human Functional pIC50 = 5.4 5.4 -30 4
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.6019/CHEMBL5442687
13052 2820 None 48 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/acs.jmedchem.3c01364
36295259 2820 None 48 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/acs.jmedchem.3c01364
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/acs.jmedchem.3c01364
53394567 79014 None 19 Human Functional pIC50 = 5.4 5.4 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 320 4 3 5 3.7 c1ccc(Nc2nc(NC3CC4CCC3C4)c3nc[nH]c3n2)cc1 10.6019/CHEMBL5442687
CHEMBL2113046 79014 None 19 Human Functional pIC50 = 5.4 5.4 - 1
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 320 4 3 5 3.7 c1ccc(Nc2nc(NC3CC4CCC3C4)c3nc[nH]c3n2)cc1 10.6019/CHEMBL5442687
170157373 195982 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 406 3 0 3 2.6 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)C2CCOCC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5414588 195982 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 406 3 0 3 2.6 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)C2CCOCC2)CC1 10.1021/acs.jmedchem.3c01364
39572558 111117 None 1 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262887 111117 None 1 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
36511613 120976 None 0 Human Functional pIC50 = 8.4 8.4 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 390 3 0 2 3.3 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)C2CCCC2)CC1 nan
CHEMBL3560365 120976 None 0 Human Functional pIC50 = 8.4 8.4 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 390 3 0 2 3.3 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)C2CCCC2)CC1 nan
39572558 111117 None 1 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262887 111117 None 1 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
209 3057 None 57 Human Functional pIC50 = 5.4 5.4 -1819 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.6019/CHEMBL5442687
2113 3057 None 57 Human Functional pIC50 = 5.4 5.4 -1819 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.6019/CHEMBL5442687
4748 3057 None 57 Human Functional pIC50 = 5.4 5.4 -1819 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.6019/CHEMBL5442687
4748.0 3057 None 57 Human Functional pIC50 = 5.4 5.4 -1819 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.6019/CHEMBL5442687
CHEMBL567 3057 None 57 Human Functional pIC50 = 5.4 5.4 -1819 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.6019/CHEMBL5442687
DB00850 3057 None 57 Human Functional pIC50 = 5.4 5.4 -1819 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.6019/CHEMBL5442687
11656002 83044 None 22 Human Functional pIC50 = 5.4 5.4 -1995 8
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 484 3 0 3 5.8 O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.6019/CHEMBL5442687
CHEMBL2181247 83044 None 22 Human Functional pIC50 = 5.4 5.4 -1995 8
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 484 3 0 3 5.8 O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.6019/CHEMBL5442687
107970 1639 None 56 Human Functional pIC50 = 5.4 5.4 -2454 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.6019/CHEMBL5442687
107970.0 1639 None 56 Human Functional pIC50 = 5.4 5.4 -2454 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.6019/CHEMBL5442687
2407 1639 None 56 Human Functional pIC50 = 5.4 5.4 -2454 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.6019/CHEMBL5442687
4167 1639 None 56 Human Functional pIC50 = 5.4 5.4 -2454 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.6019/CHEMBL5442687
CHEMBL314854 1639 None 56 Human Functional pIC50 = 5.4 5.4 -2454 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.6019/CHEMBL5442687
DB08868 1639 None 56 Human Functional pIC50 = 5.4 5.4 -2454 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.6019/CHEMBL5442687
10150497 4074 None 40 Human Functional pIC50 = 5.4 5.4 -660 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.6019/CHEMBL5442687
3240 4074 None 40 Human Functional pIC50 = 5.4 5.4 -660 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.6019/CHEMBL5442687
CHEMBL392760 4074 None 40 Human Functional pIC50 = 5.4 5.4 -660 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.6019/CHEMBL5442687
1072081 111106 None 14 Mouse Functional pIC50 = 6.4 6.4 -6 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Mouse Functional pIC50 = 6.4 6.4 -6 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
2419 3463 None 53 Human Functional pIC50 = 5.4 5.4 -7585 19
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.6019/CHEMBL5442687
5152 3463 None 53 Human Functional pIC50 = 5.4 5.4 -7585 19
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.6019/CHEMBL5442687
5152.0 3463 None 53 Human Functional pIC50 = 5.4 5.4 -7585 19
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.6019/CHEMBL5442687
559 3463 None 53 Human Functional pIC50 = 5.4 5.4 -7585 19
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.6019/CHEMBL5442687
CHEMBL1263 3463 None 53 Human Functional pIC50 = 5.4 5.4 -7585 19
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.6019/CHEMBL5442687
DB00938 3463 None 53 Human Functional pIC50 = 5.4 5.4 -7585 19
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.6019/CHEMBL5442687
86579985 111124 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262893 111124 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
86579938 111112 None 1 Mouse Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262882 111112 None 1 Mouse Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
10071196 3124 None 53 Human Functional pIC50 = 5.4 5.4 -295 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.6019/CHEMBL5442687
10071196.0 3124 None 53 Human Functional pIC50 = 5.4 5.4 -295 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.6019/CHEMBL5442687
5142 3124 None 53 Human Functional pIC50 = 5.4 5.4 -295 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.6019/CHEMBL5442687
8423 3124 None 53 Human Functional pIC50 = 5.4 5.4 -295 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.6019/CHEMBL5442687
CHEMBL2111101 3124 None 53 Human Functional pIC50 = 5.4 5.4 -295 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.6019/CHEMBL5442687
DB05316 3124 None 53 Human Functional pIC50 = 5.4 5.4 -295 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.6019/CHEMBL5442687
86579897 111108 None 0 Mouse Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
CHEMBL3262878 111108 None 0 Mouse Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
54764919 69923 None 32 Human Functional pIC50 = 5.4 5.4 -234 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 4 2 4 4.7 COc1ccncc1C(=O)NC(=O)Nc1ccc(-c2ccccc2)c(C(F)(F)F)c1 10.6019/CHEMBL5442687
CHEMBL1938952 69923 None 32 Human Functional pIC50 = 5.4 5.4 -234 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 415 4 2 4 4.7 COc1ccncc1C(=O)NC(=O)Nc1ccc(-c2ccccc2)c(C(F)(F)F)c1 10.6019/CHEMBL5442687
25074316 186476 None 25 Human Functional pIC50 = 5.4 5.4 -1 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 421 5 1 8 2.9 COC1CCN(c2cccc(-c3cc(NC(C)=O)nc(-n4nc(C)cc4C)n3)n2)CC1 10.6019/CHEMBL5442687
CHEMBL487553 186476 None 25 Human Functional pIC50 = 5.4 5.4 -1 2
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 421 5 1 8 2.9 COC1CCN(c2cccc(-c3cc(NC(C)=O)nc(-n4nc(C)cc4C)n3)n2)CC1 10.6019/CHEMBL5442687
86579897 111108 None 0 Mouse Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
CHEMBL3262878 111108 None 0 Mouse Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 5 0 3 2.6 Cc1ccc(OCC(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1C 10.1021/jm4019355
42611190 3156 None 14 Human Functional pIC50 = 5.4 5.4 -1122 21
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
5802 3156 None 14 Human Functional pIC50 = 5.4 5.4 -1122 21
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
CHEMBL1800685 3156 None 14 Human Functional pIC50 = 5.4 5.4 -1122 21
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
172463775 196831 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 435 2 1 5 1.7 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)N2CC3(CC(O)C3)C2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5432988 196831 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 435 2 1 5 1.7 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)N2CC3(CC(O)C3)C2)CC1 10.1021/acs.jmedchem.3c01364
52938427 2984 None 49 Human Functional pIC50 = 5.4 5.4 -7244 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.6019/CHEMBL5442687
52938427.0 2984 None 49 Human Functional pIC50 = 5.4 5.4 -7244 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.6019/CHEMBL5442687
5383 2984 None 49 Human Functional pIC50 = 5.4 5.4 -7244 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.6019/CHEMBL5442687
8709 2984 None 49 Human Functional pIC50 = 5.4 5.4 -7244 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.6019/CHEMBL5442687
CHEMBL3707247 2984 None 49 Human Functional pIC50 = 5.4 5.4 -7244 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.6019/CHEMBL5442687
DB12612 2984 None 49 Human Functional pIC50 = 5.4 5.4 -7244 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.6019/CHEMBL5442687
86579985 111124 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262893 111124 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
86579938 111112 None 1 Mouse Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262882 111112 None 1 Mouse Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 402 4 0 2 3.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
3954 664 None 44 Human Functional pIC50 = 5.4 5.4 -70 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 454 6 1 3 6.8 Cc1c(OCc2cccc(c2)c2ccc(cc2)C(=O)O)cc2c(c1C)C(=O)C(C2)C1CCCC1 10.6019/CHEMBL5442687
9868580 664 None 44 Human Functional pIC50 = 5.4 5.4 -70 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 454 6 1 3 6.8 Cc1c(OCc2cccc(c2)c2ccc(cc2)C(=O)O)cc2c(c1C)C(=O)C(C2)C1CCCC1 10.6019/CHEMBL5442687
CHEMBL593013 664 None 44 Human Functional pIC50 = 5.4 5.4 -70 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 454 6 1 3 6.8 Cc1c(OCc2cccc(c2)c2ccc(cc2)C(=O)O)cc2c(c1C)C(=O)C(C2)C1CCCC1 10.6019/CHEMBL5442687
172470851 197140 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 459 3 0 7 2.2 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc3c(c2)OCCO3)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5439756 197140 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 459 3 0 7 2.2 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc3c(c2)OCCO3)CC1 10.1021/acs.jmedchem.3c01364
86579939 111113 None 0 Mouse Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
CHEMBL3262883 111113 None 0 Mouse Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
135413536 448 None 58 Human Functional pIC50 = 5.4 5.4 -19054 7
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 534 6 2 5 5.0 Fc1ccc(cc1)[C@H]1[C@H](OCCN1Cc1[nH][nH]c(=O)n1)O[C@@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C 10.6019/CHEMBL5442687
230 448 None 58 Human Functional pIC50 = 5.4 5.4 -19054 7
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 534 6 2 5 5.0 Fc1ccc(cc1)[C@H]1[C@H](OCCN1Cc1[nH][nH]c(=O)n1)O[C@@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C 10.6019/CHEMBL5442687
3490 448 None 58 Human Functional pIC50 = 5.4 5.4 -19054 7
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 534 6 2 5 5.0 Fc1ccc(cc1)[C@H]1[C@H](OCCN1Cc1[nH][nH]c(=O)n1)O[C@@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C 10.6019/CHEMBL5442687
6918365 448 None 58 Human Functional pIC50 = 5.4 5.4 -19054 7
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 534 6 2 5 5.0 Fc1ccc(cc1)[C@H]1[C@H](OCCN1Cc1[nH][nH]c(=O)n1)O[C@@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C 10.6019/CHEMBL5442687
CHEMBL1471 448 None 58 Human Functional pIC50 = 5.4 5.4 -19054 7
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 534 6 2 5 5.0 Fc1ccc(cc1)[C@H]1[C@H](OCCN1Cc1[nH][nH]c(=O)n1)O[C@@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C 10.6019/CHEMBL5442687
DB00673 448 None 58 Human Functional pIC50 = 5.4 5.4 -19054 7
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 534 6 2 5 5.0 Fc1ccc(cc1)[C@H]1[C@H](OCCN1Cc1[nH][nH]c(=O)n1)O[C@@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C 10.6019/CHEMBL5442687
86579939 111113 None 0 Mouse Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
CHEMBL3262883 111113 None 0 Mouse Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 366 4 0 2 3.1 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1F 10.1021/jm4019355
73330420 120971 None 0 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 480 4 0 3 4.8 CC(C)(C)c1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 nan
CHEMBL3560209 120971 None 0 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 480 4 0 3 4.8 CC(C)(C)c1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 nan
170157378 196250 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 408 3 0 5 2.1 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)C2CCOCC2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5419703 196250 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 408 3 0 5 2.1 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)C2CCOCC2)CC1 10.1021/acs.jmedchem.3c01364
10077130 4007 None 47 Human Functional pIC50 = 5.3 5.3 -173 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.6019/CHEMBL5442687
10077130.0 4007 None 47 Human Functional pIC50 = 5.3 5.3 -173 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.6019/CHEMBL5442687
4047 4007 None 47 Human Functional pIC50 = 5.3 5.3 -173 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.6019/CHEMBL5442687
4870 4007 None 47 Human Functional pIC50 = 5.3 5.3 -173 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.6019/CHEMBL5442687
CHEMBL493982 4007 None 47 Human Functional pIC50 = 5.3 5.3 -173 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.6019/CHEMBL5442687
DB09030 4007 None 47 Human Functional pIC50 = 5.3 5.3 -173 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.6019/CHEMBL5442687
19325390 121037 None 1 Human Functional pIC50 = 6.3 6.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 3 0 2 4.1 O=C(c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
CHEMBL3561875 121037 None 1 Human Functional pIC50 = 6.3 6.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 392 3 0 2 4.1 O=C(c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
44634573 2748 None 1 Human Functional pIC50 = 5.3 5.3 -562 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442687
9168 2748 None 1 Human Functional pIC50 = 5.3 5.3 -562 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442687
CHEMBL1474387 2748 None 1 Human Functional pIC50 = 5.3 5.3 -562 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442687
CHEMBL1622930 2748 None 1 Human Functional pIC50 = 5.3 5.3 -562 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 465 6 0 2 5.0 Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2 10.6019/CHEMBL5442687
7942116 120986 None 1 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 399 4 0 4 2.2 N#Cc1ccccc1S(=O)(=O)N1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3560541 120986 None 1 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 399 4 0 4 2.2 N#Cc1ccccc1S(=O)(=O)N1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
175 3655 None 35 Human Functional pIC50 = 5.3 5.3 -15135 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.6019/CHEMBL5442687
68186 3655 None 35 Human Functional pIC50 = 5.3 5.3 -15135 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.6019/CHEMBL5442687
CHEMBL79834 3655 None 35 Human Functional pIC50 = 5.3 5.3 -15135 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.6019/CHEMBL5442687
1765 3817 None 60 Human Functional pIC50 = 5.3 5.3 -52 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.6019/CHEMBL5442687
4184 3817 None 60 Human Functional pIC50 = 5.3 5.3 -52 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.6019/CHEMBL5442687
9871419 3817 None 60 Human Functional pIC50 = 5.3 5.3 -52 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.6019/CHEMBL5442687
9871419.0 3817 None 60 Human Functional pIC50 = 5.3 5.3 -52 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.6019/CHEMBL5442687
CHEMBL398435 3817 None 60 Human Functional pIC50 = 5.3 5.3 -52 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.6019/CHEMBL5442687
DB08816 3817 None 60 Human Functional pIC50 = 5.3 5.3 -52 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.6019/CHEMBL5442687
71295864 120963 None 0 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 424 4 0 3 3.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 nan
CHEMBL3559902 120963 None 0 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 424 4 0 3 3.5 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 nan
28 3496 None 35 Human Functional pIC50 = 5.3 5.3 -1 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442687
3292447 3496 None 35 Human Functional pIC50 = 5.3 5.3 -1 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442687
CHEMBL20963 3496 None 35 Human Functional pIC50 = 5.3 5.3 -1 15
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442687
170271651 196918 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 455 4 0 4 3.4 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC23CC3)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5434815 196918 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 455 4 0 4 3.4 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC23CC3)cn1 10.1021/acs.jmedchem.3c01364
90655992 111126 None 0 Human Functional pIC50 = 8.3 8.3 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262895 111126 None 0 Human Functional pIC50 = 8.3 8.3 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
90655992 111126 None 0 Human Functional pIC50 = 8.3 8.3 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262895 111126 None 0 Human Functional pIC50 = 8.3 8.3 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
73330426 121023 None 0 Human Functional pIC50 = 8.3 8.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 486 4 0 2 5.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2C(F)(F)F)CC1 nan
CHEMBL3561495 121023 None 0 Human Functional pIC50 = 8.3 8.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 486 4 0 2 5.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2C(F)(F)F)CC1 nan
2634560 121017 None 1 Human Functional pIC50 = 8.3 8.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL3561390 121017 None 1 Human Functional pIC50 = 8.3 8.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 408 4 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
73330407 121011 None 0 Human Functional pIC50 = 8.3 8.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 378 5 0 2 3.3 CCCCC(=O)N1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
CHEMBL3561208 121011 None 0 Human Functional pIC50 = 8.3 8.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 378 5 0 2 3.3 CCCCC(=O)N1CCN(C(=O)/C=C/c2ccc(Br)cc2)CC1 nan
73330418 121028 None 0 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 426 5 0 2 4.9 CC(C)c1ccc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3561719 121028 None 0 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 426 5 0 2 4.9 CC(C)c1ccc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
86579985 111124 None 0 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262893 111124 None 0 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
71295910 121012 None 0 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 404 5 0 4 2.4 COc1cccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)c1 nan
CHEMBL3561230 121012 None 0 Human Functional pIC50 = 7.3 7.3 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 404 5 0 4 2.4 COc1cccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)c1 nan
172447297 195137 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 402 3 0 6 1.8 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cncnc2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5397313 195137 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 402 3 0 6 1.8 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cncnc2)CC1 10.1021/acs.jmedchem.3c01364
86579985 111124 None 0 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262893 111124 None 0 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 378 4 0 3 3.3 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)c(C)c3)CC2)cc1 10.1021/jm4019355
662 3680 None 7 Human Functional pIC50 = 5.3 5.3 -2 12
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 756 14 2 8 6.3 COc1ccc2c(c1)ccc(c2)S(=O)(=O)N[C@@H](c1ccc2c(c1)OCO2)CC(=O)N[C@@H](C(=O)N(C(C)C)C)Cc1ccc(cc1)CN1[C@H](C)CCC[C@@H]1C 10.6019/CHEMBL5442687
9853583 3680 None 7 Human Functional pIC50 = 5.3 5.3 -2 12
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 756 14 2 8 6.3 COc1ccc2c(c1)ccc(c2)S(=O)(=O)N[C@@H](c1ccc2c(c1)OCO2)CC(=O)N[C@@H](C(=O)N(C(C)C)C)Cc1ccc(cc1)CN1[C@H](C)CCC[C@@H]1C 10.6019/CHEMBL5442687
CHEMBL2021721 3680 None 7 Human Functional pIC50 = 5.3 5.3 -2 12
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 756 14 2 8 6.3 COc1ccc2c(c1)ccc(c2)S(=O)(=O)N[C@@H](c1ccc2c(c1)OCO2)CC(=O)N[C@@H](C(=O)N(C(C)C)C)Cc1ccc(cc1)CN1[C@H](C)CCC[C@@H]1C 10.6019/CHEMBL5442687
39572558 111117 None 1 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262887 111117 None 1 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
170156184 195377 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 4 0 4 3.2 COc1ccc(C(=O)N2CCCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5402356 195377 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 4 0 4 3.2 COc1ccc(C(=O)N2CCCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
36294314 111118 None 1 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262888 111118 None 1 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
36294314 111118 None 1 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262888 111118 None 1 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 380 5 0 4 2.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/jm4019355
9901086 187737 None 28 Human Functional pIC50 = 5.3 5.3 -4677 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442687
CHEMBL4743049 187737 None 28 Human Functional pIC50 = 5.3 5.3 -4677 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442687
CHEMBL494947 187737 None 28 Human Functional pIC50 = 5.3 5.3 -4677 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442687
1836 2592 None 44 Human Functional pIC50 = 5.3 5.3 -11220 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.6019/CHEMBL5442687
3340 2592 None 44 Human Functional pIC50 = 5.3 5.3 -11220 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.6019/CHEMBL5442687
5281040 2592 None 44 Human Functional pIC50 = 5.3 5.3 -11220 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.6019/CHEMBL5442687
5281040.0 2592 None 44 Human Functional pIC50 = 5.3 5.3 -11220 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.6019/CHEMBL5442687
CHEMBL787 2592 None 44 Human Functional pIC50 = 5.3 5.3 -11220 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.6019/CHEMBL5442687
DB00471 2592 None 44 Human Functional pIC50 = 5.3 5.3 -11220 20
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.6019/CHEMBL5442687
170157179 196546 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 4 0 4 3.2 COc1ccc(C(=O)N2CCN(C(=O)/C=C(\C)c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5426423 196546 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 4 0 4 3.2 COc1ccc(C(=O)N2CCN(C(=O)/C=C(\C)c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
172447449 195876 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 410 3 1 5 2.1 CC(C)(C)C(O)C(=O)N1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5412445 195876 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 410 3 1 5 2.1 CC(C)(C)C(O)C(=O)N1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 10.1021/acs.jmedchem.3c01364
25150014 3885 None 44 Human Functional pIC50 = 6.2 6.2 -14 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.6019/CHEMBL5442687
3952 3885 None 44 Human Functional pIC50 = 6.2 6.2 -14 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.6019/CHEMBL5442687
CHEMBL449588 3885 None 44 Human Functional pIC50 = 6.2 6.2 -14 9
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 264 3 1 1 3.4 OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C 10.6019/CHEMBL5442687
90655992 111126 None 0 Mouse Functional pIC50 = 8.2 8.2 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262895 111126 None 0 Mouse Functional pIC50 = 8.2 8.2 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
90655992 111126 None 0 Mouse Functional pIC50 = 8.2 8.2 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
CHEMBL3262895 111126 None 0 Mouse Functional pIC50 = 8.2 8.2 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 440 3 0 3 3.4 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3c(c2)CCO3)CC1 10.1021/jm4019355
73169083 120974 None 29 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. Dose-response characterization of small molecule antagonists of the EBI2 receptor via a chemotaxis assay. (Class of assay: confirmatory) PubChem BioAssay. Dose-response characterization of small molecule antagonists of the EBI2 receptor via a chemotaxis assay. (Class of assay: confirmatory)
ChEMBL 418 4 0 2 4.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
CHEMBL3560331 120974 None 29 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. Dose-response characterization of small molecule antagonists of the EBI2 receptor via a chemotaxis assay. (Class of assay: confirmatory) PubChem BioAssay. Dose-response characterization of small molecule antagonists of the EBI2 receptor via a chemotaxis assay. (Class of assay: confirmatory)
ChEMBL 418 4 0 2 4.5 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
73330417 120965 None 0 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 412 4 0 2 4.4 Cc1cc(C)cc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)c1 nan
CHEMBL3559986 120965 None 0 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 412 4 0 2 4.4 Cc1cc(C)cc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)c1 nan
2674674 51251 None 4 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory) PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory)
ChEMBL 400 5 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL1580410 51251 None 4 Human Functional pIC50 = 8.2 8.2 - 1
PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory) PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory)
ChEMBL 400 5 0 3 3.0 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)/C=C/c2ccccc2)CC1 nan
168228701 197095 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 437 3 1 2 3.9 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5438584 197095 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 437 3 1 2 3.9 O=C(/C=C/c1ccc(Br)cc1)N1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1 10.1021/acs.jmedchem.3c01364
6258671 48685 None 3 Human Functional pIC50 = 6.2 6.2 - 1
PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory) PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory)
ChEMBL 374 4 0 3 2.4 O=C(/C=C/c1ccccc1)N1CCN(S(=O)(=O)c2ccc(F)cc2)CC1 nan
CHEMBL1557734 48685 None 3 Human Functional pIC50 = 6.2 6.2 - 1
PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory) PubChem BioAssay. Dose-response confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assay. (Class of assay: confirmatory)
ChEMBL 374 4 0 3 2.4 O=C(/C=C/c1ccccc1)N1CCN(S(=O)(=O)c2ccc(F)cc2)CC1 nan
119192 2481 None 38 Human Functional pIC50 = 5.2 5.2 -81 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC 10.6019/CHEMBL5442687
1582 2481 None 38 Human Functional pIC50 = 5.2 5.2 -81 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC 10.6019/CHEMBL5442687
CHEMBL506981 2481 None 38 Human Functional pIC50 = 5.2 5.2 -81 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC 10.6019/CHEMBL5442687
DB06455 2481 None 38 Human Functional pIC50 = 5.2 5.2 -81 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC 10.6019/CHEMBL5442687
276 3513 None 37 Human Functional pIC50 = 5.2 5.2 -3162 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.6019/CHEMBL5442687
5312149 3513 None 37 Human Functional pIC50 = 5.2 5.2 -3162 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.6019/CHEMBL5442687
CHEMBL431298 3513 None 37 Human Functional pIC50 = 5.2 5.2 -3162 5
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.6019/CHEMBL5442687
130 3500 None 32 Human Functional pIC50 = 5.2 5.2 -3235 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442687
3378093 3500 None 32 Human Functional pIC50 = 5.2 5.2 -3235 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442687
CHEMBL281350 3500 None 32 Human Functional pIC50 = 5.2 5.2 -3235 10
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442687
172440550 195300 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 382 3 1 5 1.5 CC(C)(O)C(=O)N1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5400278 195300 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 382 3 1 5 1.5 CC(C)(O)C(=O)N1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 10.1021/acs.jmedchem.3c01364
39572558 111117 None 1 Mouse Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262887 111117 None 1 Mouse Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C)cc3)CC2)cc1 10.1021/jm4019355
73330400 120962 None 0 Human Functional pIC50 = 7.2 7.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 530 4 0 3 3.9 O=C(/C=C/c1ccc(Br)cc1F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3559896 120962 None 0 Human Functional pIC50 = 7.2 7.2 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 530 4 0 3 3.9 O=C(/C=C/c1ccc(Br)cc1F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
170157372 195038 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 476 7 0 8 1.8 COCCOc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5395361 195038 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 476 7 0 8 1.8 COCCOc1ncc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)cn1 10.1021/acs.jmedchem.3c01364
1209 1658 None 52 Human Functional pIC50 = 5.2 5.2 -54 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
203 1658 None 52 Human Functional pIC50 = 5.2 5.2 -54 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
3386 1658 None 52 Human Functional pIC50 = 5.2 5.2 -54 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
CHEMBL41 1658 None 52 Human Functional pIC50 = 5.2 5.2 -54 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
DB00472 1658 None 52 Human Functional pIC50 = 5.2 5.2 -54 25
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442687
86579942 111116 None 0 Human Functional pIC50 = 7.2 7.2 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262886 111116 None 0 Human Functional pIC50 = 7.2 7.2 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
71450251 83023 None 29 Human Functional pIC50 = 5.2 5.2 -9332 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 399 4 0 4 5.1 Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.6019/CHEMBL5442687
CHEMBL2181226 83023 None 29 Human Functional pIC50 = 5.2 5.2 -9332 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 399 4 0 4 5.1 Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.6019/CHEMBL5442687
8868 3547 None 23 Human Functional pIC50 = 5.2 5.2 -562 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.6019/CHEMBL5442687
9887077 3547 None 23 Human Functional pIC50 = 5.2 5.2 -562 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.6019/CHEMBL5442687
CHEMBL513136 3547 None 23 Human Functional pIC50 = 5.2 5.2 -562 3
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.6019/CHEMBL5442687
13052 2820 None 48 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
13052 2820 None 48 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
2634530 120966 None 3 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 388 4 0 3 2.7 Cc1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
CHEMBL3559987 120966 None 3 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 388 4 0 3 2.7 Cc1ccc(S(=O)(=O)N2CCN(C(=O)/C=C/c3ccc(F)cc3)CC2)cc1 nan
172439578 195307 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 441 3 1 6 2.3 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc3[nH]ncc3c2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5400459 195307 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 441 3 1 6 2.3 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc3[nH]ncc3c2)CC1 10.1021/acs.jmedchem.3c01364
172441945 195037 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 470 3 0 6 2.8 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(C(F)(F)F)nc2)CC1 10.1021/acs.jmedchem.3c01364
CHEMBL5395357 195037 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 470 3 0 6 2.8 O=C(/C=C/c1ccc2c(c1)OC(F)(F)O2)N1CCN(C(=O)c2cnc(C(F)(F)F)nc2)CC1 10.1021/acs.jmedchem.3c01364
86579940 111114 None 0 Mouse Functional pIC50 = 7.2 7.2 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262884 111114 None 0 Mouse Functional pIC50 = 7.2 7.2 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
86579942 111116 None 0 Human Functional pIC50 = 7.2 7.2 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262886 111116 None 0 Human Functional pIC50 = 7.2 7.2 1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
172447991 195911 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 404 3 0 6 1.7 Cn1cnc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)c1 10.1021/acs.jmedchem.3c01364
CHEMBL5413214 195911 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 404 3 0 6 1.7 Cn1cnc(C(=O)N2CCN(C(=O)/C=C/c3ccc4c(c3)OC(F)(F)O4)CC2)c1 10.1021/acs.jmedchem.3c01364
73330395 121003 None 0 Human Functional pIC50 = 6.1 6.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 530 4 0 3 3.9 O=C(/C=C/c1cc(Br)ccc1F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
CHEMBL3560891 121003 None 0 Human Functional pIC50 = 6.1 6.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 530 4 0 3 3.9 O=C(/C=C/c1cc(Br)ccc1F)N1CCN(S(=O)(=O)c2ccc(Br)cc2)CC1 nan
86579942 111116 None 0 Mouse Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262886 111116 None 0 Mouse Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
32268755 120985 None 2 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccccc2Br)CC1 nan
CHEMBL3560529 120985 None 2 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 452 4 0 3 3.1 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2ccccc2Br)CC1 nan
73330419 121021 None 0 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 436 4 0 2 4.6 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2F)CC1 nan
CHEMBL3561484 121021 None 0 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 436 4 0 2 4.6 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(Cl)cc2F)CC1 nan
73330399 121029 None 0 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 470 4 0 2 5.0 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(F)cc2C(F)(F)F)CC1 nan
CHEMBL3561739 121029 None 0 Human Functional pIC50 = 8.1 8.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 470 4 0 2 5.0 O=C(/C=C/c1ccc(Br)cc1)N1CCN(Cc2ccc(F)cc2C(F)(F)F)CC1 nan
13052 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
13052 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysisAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
13052 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
86579941 111115 None 1 Mouse Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262885 111115 None 1 Mouse Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
8924480 120984 None 0 Human Functional pIC50 = 7.1 7.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 380 4 0 4 2.4 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccs2)CC1 nan
CHEMBL3560506 120984 None 0 Human Functional pIC50 = 7.1 7.1 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 380 4 0 4 2.4 O=C(/C=C/c1ccc(F)cc1)N1CCN(S(=O)(=O)c2cccs2)CC1 nan
86579941 111115 None 1 Mouse Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262885 111115 None 1 Mouse Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
170156216 195554 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 4 0 4 3.2 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2C)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5405959 195554 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 4 0 4 3.2 COc1ccc(C(=O)N2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2C)cn1 10.1021/acs.jmedchem.3c01364
456214 87380 None 43 Human Functional pIC50 = 5.1 5.1 -660 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 388 7 3 7 4.2 CC(C)[C@H](CO)Nc1nc(Nc2cccc(Cl)c2)c2ncn(C(C)C)c2n1 10.6019/CHEMBL5442687
CHEMBL23327 87380 None 43 Human Functional pIC50 = 5.1 5.1 -660 6
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
ChEMBL 388 7 3 7 4.2 CC(C)[C@H](CO)Nc1nc(Nc2cccc(Cl)c2)c2ncn(C(C)C)c2n1 10.6019/CHEMBL5442687
1072081 111106 None 14 Human Functional pIC50 = 7.1 7.1 6 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Functional pIC50 = 7.1 7.1 6 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86579940 111114 None 0 Mouse Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
CHEMBL3262884 111114 None 0 Mouse Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 364 4 0 3 3.0 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3cccc(C)c3)CC2)cc1 10.1021/jm4019355
170156068 195808 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 5 1 4 3.3 COc1ccc(C(=O)NC2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
CHEMBL5411108 195808 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assayAntagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
ChEMBL 443 5 1 4 3.3 COc1ccc(C(=O)NC2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cn1 10.1021/acs.jmedchem.3c01364
13052 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
73330397 120957 None 0 Human Functional pIC50 = 8.0 8.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 440 4 0 2 5.1 CC(C)(C)c1ccc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3559757 120957 None 0 Human Functional pIC50 = 8.0 8.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 440 4 0 2 5.1 CC(C)(C)c1ccc(CN2CCN(C(=O)/C=C/c3ccc(Br)cc3)CC2)cc1 nan
26867544 121007 None 0 Human Functional pIC50 = 8.0 8.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 464 5 0 4 3.0 COc1ccc(/C=C/C(=O)N2CCN(S(=O)(=O)c3ccc(Br)cc3)CC2)cc1 nan
CHEMBL3561084 121007 None 0 Human Functional pIC50 = 8.0 8.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 464 5 0 4 3.0 COc1ccc(/C=C/C(=O)N2CCN(S(=O)(=O)c3ccc(Br)cc3)CC2)cc1 nan
1072081 111106 None 14 Human Functional pIC50 = 7.0 7.0 6 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Functional pIC50 = 7.0 7.0 6 2
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assayAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86579902 111110 None 1 Mouse Functional pIC50 = 7.0 7.0 -4 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262880 111110 None 1 Mouse Functional pIC50 = 7.0 7.0 -4 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579902 111110 None 1 Mouse Functional pIC50 = 7.0 7.0 -4 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262880 111110 None 1 Mouse Functional pIC50 = 7.0 7.0 -4 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 348 4 0 2 2.9 Cc1ccc(/C=C/C(=O)N2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1021/jm4019355
86579942 111116 None 0 Mouse Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262886 111116 None 0 Mouse Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 428 4 0 3 3.5 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(Br)cc3)CC2)cc1 10.1021/jm4019355
86579941 111115 None 1 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262885 111115 None 1 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
1072066 20311 None 13 Mouse Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL1305842 20311 None 13 Mouse Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
1072066 20311 None 13 Mouse Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL1305842 20311 None 13 Mouse Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 372 5 0 3 2.6 O=C(COc1ccc(Cl)cc1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
86579941 111115 None 1 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
CHEMBL3262885 111115 None 1 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assayAntagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
ChEMBL 418 4 0 3 3.7 COc1ccc(/C=C/C(=O)N2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1021/jm4019355
26756555 121362 None 1 Human Functional pIC50 = 7.0 7.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 340 4 0 2 3.7 O=C(/C=C/c1ccccc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
CHEMBL3561800 121362 None 1 Human Functional pIC50 = 7.0 7.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 340 4 0 2 3.7 O=C(/C=C/c1ccccc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
CHEMBL3580408 121362 None 1 Human Functional pIC50 = 7.0 7.0 - 1
PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory) PubChem BioAssay. SAR confirmation of small molecule antagonists of the EBI2 receptor via a luminescent beta-arrestin assa. (Class of assay: confirmatory)
ChEMBL 340 4 0 2 3.7 O=C(/C=C/c1ccccc1)N1CCN(Cc2ccc(Cl)cc2)CC1 nan
13051 2821 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Measuring intracellular calcium release as detected using a FLIPR-type assay.Measuring intracellular calcium release as detected using a FLIPR-type assay.
Guide to Pharmacology 440 6 0 3 5.4 C1=CC(=CN=C1)CN(CC2=C(C=C(C=C2)Cl)Cl)S(=O)(=O)C3=CC=C(C=C3)Cl 24678947
13051 2821 None 0 Mouse Functional pEC50 = 5.7 5.7 -1 2
Measuring intracellular calcium release as detected using a FLIPR-type assay.Measuring intracellular calcium release as detected using a FLIPR-type assay.
Guide to Pharmacology 440 6 0 3 5.4 C1=CC(=CN=C1)CN(CC2=C(C=C(C=C2)Cl)Cl)S(=O)(=O)C3=CC=C(C=C3)Cl 24678947
2726776 2821 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Measuring intracellular calcium release as detected using a FLIPR-type assay.Measuring intracellular calcium release as detected using a FLIPR-type assay.
Guide to Pharmacology 440 6 0 3 5.4 C1=CC(=CN=C1)CN(CC2=C(C=C(C=C2)Cl)Cl)S(=O)(=O)C3=CC=C(C=C3)Cl 24678947
2726776 2821 None 0 Mouse Functional pEC50 = 5.7 5.7 -1 2
Measuring intracellular calcium release as detected using a FLIPR-type assay.Measuring intracellular calcium release as detected using a FLIPR-type assay.
Guide to Pharmacology 440 6 0 3 5.4 C1=CC(=CN=C1)CN(CC2=C(C=C(C=C2)Cl)Cl)S(=O)(=O)C3=CC=C(C=C3)Cl 24678947
123976 51 None 0 Human Functional pEC50 = 5.5 5.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 6 2 2 6.4 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
2752 51 None 0 Human Functional pEC50 = 5.5 5.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 6 2 2 6.4 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
CHEMBL353882 51 None 0 Human Functional pEC50 = 5.5 5.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 6 2 2 6.4 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
4352 179 None 0 Human Functional pEC50 = 5.8 5.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
473141 179 None 0 Human Functional pEC50 = 5.8 5.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
CHEMBL497834 179 None 0 Human Functional pEC50 = 5.8 5.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
DB04706 179 None 0 Human Functional pEC50 = 5.8 5.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
2885 50 None 0 Human Functional pEC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.5 O[C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)C1)C 21796211
65094 50 None 0 Human Functional pEC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.5 O[C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)C1)C 21796211
CHEMBL169046 50 None 0 Human Functional pEC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.5 O[C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)C1)C 21796211
DB04705 50 None 0 Human Functional pEC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.5 O[C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)C1)C 21796211
107722 170 None 32 Human Functional pEC50 = 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
4351 170 None 32 Human Functional pEC50 = 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
CHEMBL497207 170 None 32 Human Functional pEC50 = 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 402 5 2 2 6.4 CC(CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
4354 178 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 3 5.3 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
52931518 178 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 3 5.3 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
4355 177 None 13 Human Functional pEC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
473142 177 None 13 Human Functional pEC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
CHEMBL3311219 177 None 13 Human Functional pEC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
15907756 167 None 0 Human Functional pEC50 = 8.9 8.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 3 5.3 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
4353 167 None 0 Human Functional pEC50 = 8.9 8.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 3 5.3 OC[C@@H](CCC[C@H]([C@H]1CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2[C@H](O)C=C2[C@]1(C)CC[C@@H](C2)O)C)C 21796211
11954197 166 None 27 Human Functional pEC50 = 9.0 9.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
11954197 166 None 27 Human Functional pEC50 = 9.0 9.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796212
4350 166 None 27 Human Functional pEC50 = 9.0 9.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
4350 166 None 27 Human Functional pEC50 = 9.0 9.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796212
CHEMBL4788348 166 None 27 Human Functional pEC50 = 9.0 9.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
CHEMBL4788348 166 None 27 Human Functional pEC50 = 9.0 9.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796212
13050 1071 None 6 Human Functional pIC50 = 8.1 8.1 - 1
Antagonism of β-arrestin recruitmentAntagonism of β-arrestin recruitment
Guide to Pharmacology 432 4 0 7 1.8 FC1(OC2=C(O1)C=CC(=C2)/C=C/C(N3CCN(C(C4=CN=C(OC)N=C4)=O)CC3)=O)F 38047891
169494480 1071 None 6 Human Functional pIC50 = 8.1 8.1 - 1
Antagonism of β-arrestin recruitmentAntagonism of β-arrestin recruitment
Guide to Pharmacology 432 4 0 7 1.8 FC1(OC2=C(O1)C=CC(=C2)/C=C/C(N3CCN(C(C4=CN=C(OC)N=C4)=O)CC3)=O)F 38047891
CHEMBL5394700 1071 None 6 Human Functional pIC50 = 8.1 8.1 - 1
Antagonism of β-arrestin recruitmentAntagonism of β-arrestin recruitment
Guide to Pharmacology 432 4 0 7 1.8 FC1(OC2=C(O1)C=CC(=C2)/C=C/C(N3CCN(C(C4=CN=C(OC)N=C4)=O)CC3)=O)F 38047891
13052 2820 None 48 Mouse Functional pIC50 = 7.8 7.8 -3 2
Antagonism of NIBR51-induced GPR183 activationAntagonism of NIBR51-induced GPR183 activation
Guide to Pharmacology 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 24678947
36295259 2820 None 48 Mouse Functional pIC50 = 7.8 7.8 -3 2
Antagonism of NIBR51-induced GPR183 activationAntagonism of NIBR51-induced GPR183 activation
Guide to Pharmacology 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 24678947
CHEMBL3262896 2820 None 48 Mouse Functional pIC50 = 7.8 7.8 -3 2
Antagonism of NIBR51-induced GPR183 activationAntagonism of NIBR51-induced GPR183 activation
Guide to Pharmacology 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 24678947
13052 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonism of NIBR51-induced GPR183 activationAntagonism of NIBR51-induced GPR183 activation
Guide to Pharmacology 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 24678947
36295259 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonism of NIBR51-induced GPR183 activationAntagonism of NIBR51-induced GPR183 activation
Guide to Pharmacology 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 24678947
CHEMBL3262896 2820 None 48 Human Functional pIC50 = 8.0 8.0 3 2
Antagonism of NIBR51-induced GPR183 activationAntagonism of NIBR51-induced GPR183 activation
Guide to Pharmacology 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 24678947
126843232 1885 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Determined in a CREB-based reporter assay in HEK293 cells transiently transfected with wild type hGPR183; measuring inhibition of GPR183 constitutive activity.Determined in a CREB-based reporter assay in HEK293 cells transiently transfected with wild type hGPR183; measuring inhibition of GPR183 constitutive activity.
Guide to Pharmacology 478 4 0 3 5.7 C1CN(CCC12CN(C(=O)O2)CC3=CC(=C(C=C3)Cl)Cl)C(=O)/C=C/C4=CC=C(C=C4)Cl 21673108
13053 1885 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Determined in a CREB-based reporter assay in HEK293 cells transiently transfected with wild type hGPR183; measuring inhibition of GPR183 constitutive activity.Determined in a CREB-based reporter assay in HEK293 cells transiently transfected with wild type hGPR183; measuring inhibition of GPR183 constitutive activity.
Guide to Pharmacology 478 4 0 3 5.7 C1CN(CCC12CN(C(=O)O2)CC3=CC(=C(C=C3)Cl)Cl)C(=O)/C=C/C4=CC=C(C=C4)Cl 21673108
11954197 166 None 27 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
11954197 166 None 27 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796212
4350 166 None 27 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
4350 166 None 27 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796212
CHEMBL4788348 166 None 27 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796211
CHEMBL4788348 166 None 27 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 418 5 3 3 5.5 O[C@H]1CC[C@]2(C(=C[C@H]([C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)O)C1)C 21796212


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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
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13052 2820 None 48 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
13052 2820 None 48 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
36295259 2820 None 48 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
CHEMBL3262896 2820 None 48 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 428 4 0 3 3.5 COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)/C=C/C3=CC=C(C=C3)Br 10.1021/jm4019355
1072081 111106 None 14 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
1072081 111106 None 14 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysisAntagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
1072081 111106 None 14 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysisDisplacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysisDisplacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
1072081 111106 None 14 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysisDisplacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
CHEMBL3262876 111106 None 14 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysisDisplacement of [3H]-7-alpha,25-OHC from recombinant human EBI2 receptor expressed in CHO cells after 10 mins by scintillation counting analysis
ChEMBL 388 5 0 3 3.1 O=C(COc1ccc2ccccc2c1)N1CCN(C(=O)Cc2ccccc2)CC1 10.1021/jm4019355
126843232 1885 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Measuring inhibition of [<sup>35</sup>S]GTP&gamma;S binding to hGPR183 in cell membrane preparationsMeasuring inhibition of [<sup>35</sup>S]GTP&gamma;S binding to hGPR183 in cell membrane preparations
Guide to Pharmacology 478 4 0 3 5.7 C1CN(CCC12CN(C(=O)O2)CC3=CC(=C(C=C3)Cl)Cl)C(=O)/C=C/C4=CC=C(C=C4)Cl 21673108
13053 1885 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Measuring inhibition of [<sup>35</sup>S]GTP&gamma;S binding to hGPR183 in cell membrane preparationsMeasuring inhibition of [<sup>35</sup>S]GTP&gamma;S binding to hGPR183 in cell membrane preparations
Guide to Pharmacology 478 4 0 3 5.7 C1CN(CCC12CN(C(=O)O2)CC3=CC(=C(C=C3)Cl)Cl)C(=O)/C=C/C4=CC=C(C=C4)Cl 21673108