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
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 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
11272103 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL363840 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
11272103 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.087
CHEMBL363840 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.087
11272103 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil at 30 nMAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil at 30 nM
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.087
CHEMBL363840 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil at 30 nMAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil at 30 nM
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.087
11272103 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL363840 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
11272103 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Human Functional pIC50 = 11 11.0 -37 8
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44455820 95495 None 0 Human Functional pIC50 = 11.0 11.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 551 11 3 7 4.9 CCC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257074 95495 None 0 Human Functional pIC50 = 11.0 11.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 551 11 3 7 4.9 CCC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
10458976 95064 None 0 Human Functional pIC50 = 10.9 10.9 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 509 9 3 7 3.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254930 95064 None 0 Human Functional pIC50 = 10.9 10.9 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 509 9 3 7 3.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44455711 168836 None 0 Human Functional pIC50 = 10.9 10.9 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 509 9 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL437031 168836 None 0 Human Functional pIC50 = 10.9 10.9 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 509 9 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11340670 127301 None 0 Human Functional pIC50 = 10.8 10.8 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 483 7 2 3 5.8 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)ccc1F 10.1021/jm049530m
CHEMBL365820 127301 None 0 Human Functional pIC50 = 10.8 10.8 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 483 7 2 3 5.8 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)ccc1F 10.1021/jm049530m
11328714 79029 None 0 Human Functional pIC50 = 10.8 10.8 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113074 79029 None 0 Human Functional pIC50 = 10.8 10.8 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44455686 95545 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 523 9 3 7 4.3 CC(C)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257293 95545 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 523 9 3 7 4.3 CC(C)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455869 97598 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 507 9 2 7 4.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270582 97598 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 507 9 2 7 4.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455509 166521 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 493 9 2 6 4.4 CCc1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL427728 166521 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 493 9 2 6 4.4 CCc1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455485 155588 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 507 9 2 6 5.0 CC(C)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL404122 155588 None 0 Human Functional pIC50 = 10.7 10.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 507 9 2 6 5.0 CC(C)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11329244 71140 None 6 Human Functional pIC50 = 10.5 10.5 20 7
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL195433 71140 None 6 Human Functional pIC50 = 10.5 10.5 20 7
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11329244 71140 None 6 Human Functional pIC50 = 10.5 10.5 20 7
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71140 None 6 Human Functional pIC50 = 10.5 10.5 20 7
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11227406 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL250689 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
11227406 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Antagonist activity at CCR3 assessed as inhibition of chemotaxis by cell based assayAntagonist activity at CCR3 assessed as inhibition of chemotaxis by cell based assay
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm300682j
CHEMBL250689 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Antagonist activity at CCR3 assessed as inhibition of chemotaxis by cell based assayAntagonist activity at CCR3 assessed as inhibition of chemotaxis by cell based assay
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm300682j
11227406 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL250689 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
11227406 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL250689 94398 None 2 Human Functional pIC50 = 10.5 10.5 107 4
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
10050884 154742 None 15 Human Functional pIC50 = 10.4 10.4 -1 3
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.087
CHEMBL399495 154742 None 15 Human Functional pIC50 = 10.4 10.4 -1 3
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.087
11227406 94398 None 2 Human Functional pIC50 = 10.4 10.4 107 4
Inhibition of eotaxin-induced chemotaxis of Cynomolgus monkey eosinophilsInhibition of eotaxin-induced chemotaxis of Cynomolgus monkey eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL250689 94398 None 2 Human Functional pIC50 = 10.4 10.4 107 4
Inhibition of eotaxin-induced chemotaxis of Cynomolgus monkey eosinophilsInhibition of eotaxin-induced chemotaxis of Cynomolgus monkey eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
10050884 154742 None 15 Human Functional pIC50 = 10.4 10.4 -1 3
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL399495 154742 None 15 Human Functional pIC50 = 10.4 10.4 -1 3
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
11169258 140984 None 0 Human Functional pIC50 = 10.4 10.4 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 587 8 2 10 3.8 Cn1nnnc1-c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1021/jm049530m
CHEMBL382108 140984 None 0 Human Functional pIC50 = 10.4 10.4 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 587 8 2 10 3.8 Cn1nnnc1-c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1021/jm049530m
11488078 79032 None 0 Human Functional pIC50 = 10.4 10.4 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113077 79032 None 0 Human Functional pIC50 = 10.4 10.4 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44455683 155178 None 0 Human Functional pIC50 = 10.3 10.3 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 531 9 3 7 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL401879 155178 None 0 Human Functional pIC50 = 10.3 10.3 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 531 9 3 7 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
44455745 155391 None 0 Human Functional pIC50 = 10.3 10.3 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 559 8 3 7 4.0 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(Br)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL402983 155391 None 0 Human Functional pIC50 = 10.3 10.3 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 559 8 3 7 4.0 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(Br)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455793 95280 None 0 Human Functional pIC50 = 10.2 10.2 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 483 9 3 5 4.4 CC(=O)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL256068 95280 None 0 Human Functional pIC50 = 10.2 10.2 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 483 9 3 5 4.4 CC(=O)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
11397114 133537 None 0 Human Functional pIC50 = 10.2 10.2 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2cn[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL3706810 133537 None 0 Human Functional pIC50 = 10.2 10.2 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2cn[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44455766 95738 None 0 Human Functional pIC50 = 10.2 10.2 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 479 8 2 6 4.3 C[C@H](C[C@@H](C)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL258156 95738 None 0 Human Functional pIC50 = 10.2 10.2 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 479 8 2 6 4.3 C[C@H](C[C@@H](C)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11953409 94269 None 0 Human Functional pIC50 = 10.2 10.2 7 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249854 94269 None 0 Human Functional pIC50 = 10.2 10.2 7 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445847 94477 None 0 Human Functional pIC50 = 10.1 10.1 - 1
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CNCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251079 94477 None 0 Human Functional pIC50 = 10.1 10.1 - 1
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CNCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11214474 71377 None 0 Human Functional pIC50 = 10.1 10.1 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 514 6 2 4 6.7 O=C(Nc1nc2c(Cl)cccc2s1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL195790 71377 None 0 Human Functional pIC50 = 10.1 10.1 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 514 6 2 4 6.7 O=C(Nc1nc2c(Cl)cccc2s1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44445845 94295 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CCNC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL250056 94295 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CCNC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455845 97512 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 537 10 3 7 4.5 CC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270146 97512 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 537 10 3 7 4.5 CC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
44455846 97513 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 515 9 2 6 5.1 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270147 97513 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 515 9 2 6 5.1 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
44455458 167555 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 533 9 3 7 5.3 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2ccon2)cc(-c2ccon2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL429846 167555 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 533 9 3 7 5.3 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2ccon2)cc(-c2ccon2)c1 10.1016/j.bmcl.2007.11.067
11454941 71166 None 0 Human Functional pIC50 = 10 10.0 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 505 7 2 6 4.7 Cc1nnnn1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL195555 71166 None 0 Human Functional pIC50 = 10 10.0 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 505 7 2 6 4.7 Cc1nnnn1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
10050884 154742 None 15 Crab-eating macaque Functional pIC50 = 9.8 9.8 1 3
Antagonist activity at CCR3 receptor in cynomolgus monkey eosinophil assessed as as inhibition of chemotaxisAntagonist activity at CCR3 receptor in cynomolgus monkey eosinophil assessed as as inhibition of chemotaxis
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL399495 154742 None 15 Crab-eating macaque Functional pIC50 = 9.8 9.8 1 3
Antagonist activity at CCR3 receptor in cynomolgus monkey eosinophil assessed as as inhibition of chemotaxisAntagonist activity at CCR3 receptor in cynomolgus monkey eosinophil assessed as as inhibition of chemotaxis
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
44455459 95144 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL255398 95144 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
10140602 166713 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 479 7 2 6 3.4 C[C@H](CC(=O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL428071 166713 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 479 7 2 6 3.4 C[C@H](CC(=O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11398022 98684 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
CHEMBL277131 98684 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
44455484 167502 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 493 9 2 6 4.6 CC(C)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL429604 167502 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 493 9 2 6 4.6 CC(C)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455483 97882 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 537 10 3 7 3.8 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)(C)C(=O)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL272068 97882 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 537 10 3 7 3.8 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)(C)C(=O)O)c1 10.1016/j.bmcl.2007.11.067
11385766 132864 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL370082 132864 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11236950 94817 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 479 9 2 6 4.3 CN(CCCc1ccc(F)cc1)C[C@@H]1CCCC[C@H]1NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL253210 94817 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 479 9 2 6 4.3 CN(CCCc1ccc(F)cc1)C[C@@H]1CCCC[C@H]1NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
71460523 81525 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CCR3 receptor in human eosinophils assessed as inhibition of CCL11-induced degranulation after 4 hrs by ELISAAntagonist activity at CCR3 receptor in human eosinophils assessed as inhibition of CCL11-induced degranulation after 4 hrs by ELISA
ChEMBL 423 7 3 4 3.7 O=C(Nc1ccccc1OCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160099 81525 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CCR3 receptor in human eosinophils assessed as inhibition of CCL11-induced degranulation after 4 hrs by ELISAAntagonist activity at CCR3 receptor in human eosinophils assessed as inhibition of CCL11-induced degranulation after 4 hrs by ELISA
ChEMBL 423 7 3 4 3.7 O=C(Nc1ccccc1OCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
44455817 155268 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 538 9 3 8 3.6 CNC(=O)O[C@H](C[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)N1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL402331 155268 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 538 9 3 8 3.6 CNC(=O)O[C@H](C[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)N1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
10050884 154742 None 15 Human Functional pIC50 = 9.1 9.1 -1 3
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-stimulated intracellular calcium fluxAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-stimulated intracellular calcium flux
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL399495 154742 None 15 Human Functional pIC50 = 9.1 9.1 -1 3
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-stimulated intracellular calcium fluxAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-stimulated intracellular calcium flux
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
44445854 94136 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 522 7 2 7 3.3 CC(=O)c1sc(NC(=O)N[C@@H]2CS(=O)(=O)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249057 94136 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in human eosinophils
ChEMBL 522 7 2 7 3.3 CC(=O)c1sc(NC(=O)N[C@@H]2CS(=O)(=O)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
45267588 198490 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 5 2 4 4.5 Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c(O)c1 10.1016/j.bmc.2009.06.066
CHEMBL560275 198490 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 5 2 4 4.5 Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c(O)c1 10.1016/j.bmc.2009.06.066
44512617 197794 None 0 Human Functional pIC50 = 9 9.0 79 2
Antagonist activity at human CCR3 expressed in mouse B300-19 cells by functional inhibition curve analysisAntagonist activity at human CCR3 expressed in mouse B300-19 cells by functional inhibition curve analysis
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL551735 197794 None 0 Human Functional pIC50 = 9 9.0 79 2
Antagonist activity at human CCR3 expressed in mouse B300-19 cells by functional inhibition curve analysisAntagonist activity at human CCR3 expressed in mouse B300-19 cells by functional inhibition curve analysis
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44455658 167369 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 479 8 3 5 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nccn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL429323 167369 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 479 8 3 5 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nccn2C)c1 10.1016/j.bmcl.2007.11.067
44289715 170338 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 465 8 2 6 3.8 Cc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL444568 170338 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 465 8 2 6 3.8 Cc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11272103 124442 None 0 Human Functional pIC50 = 9 9.0 -37 8
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Human Functional pIC50 = 9 9.0 -37 8
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11363006 70459 None 0 Human Functional pIC50 = 9 9.0 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 453 7 2 3 5.5 COc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
CHEMBL194601 70459 None 0 Human Functional pIC50 = 9 9.0 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 453 7 2 3 5.5 COc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
44455539 167078 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 465 8 2 6 3.9 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL428775 167078 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 465 8 2 6 3.9 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
45271892 197796 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 515 5 1 5 4.3 O=C(C=C1CCN(C(=O)c2ccc3c(c2)OCO3)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL551739 197796 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 515 5 1 5 4.3 O=C(C=C1CCN(C(=O)c2ccc3c(c2)OCO3)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
71460523 81525 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 423 7 3 4 3.7 O=C(Nc1ccccc1OCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160099 81525 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 423 7 3 4 3.7 O=C(Nc1ccccc1OCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
45271891 197795 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 6 1 4 4.5 COc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)cc1 10.1016/j.bmc.2009.06.066
CHEMBL551738 197795 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 6 1 4 4.5 COc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)cc1 10.1016/j.bmc.2009.06.066
11363005 60526 None 0 Human Functional pIC50 = 8 8.0 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 453 7 2 3 5.5 COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL175634 60526 None 0 Human Functional pIC50 = 8 8.0 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 453 7 2 3 5.5 COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11329244 71140 None 6 Mouse Functional pIC50 = 8 8.0 -20 7
Inhibition of eotaxin-induced chemotaxis of mouse eosinophilsInhibition of eotaxin-induced chemotaxis of mouse eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71140 None 6 Mouse Functional pIC50 = 8 8.0 -20 7
Inhibition of eotaxin-induced chemotaxis of mouse eosinophilsInhibition of eotaxin-induced chemotaxis of mouse eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
45269392 198482 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 374 5 1 2 4.4 O=C(/C=C/c1ccccc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL560198 198482 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 374 5 1 2 4.4 O=C(/C=C/c1ccccc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
71449694 81529 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 437 8 3 4 3.9 O=C(Nc1ccccc1COCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160102 81529 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 437 8 3 4 3.9 O=C(Nc1ccccc1COCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
70694703 76174 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 578 5 2 3 6.1 O=C(Nc1cccc(Br)c1)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2057764 76174 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 578 5 2 3 6.1 O=C(Nc1cccc(Br)c1)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
44451981 161365 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 454 6 1 3 6.2 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2007.10.003
CHEMBL412061 161365 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 454 6 1 3 6.2 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2007.10.003
44282031 119879 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 488 8 2 5 3.2 CC(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)N1CCCC1 10.1016/s0960-894x(01)00249-9
CHEMBL34839 119879 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 488 8 2 5 3.2 CC(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)N1CCCC1 10.1016/s0960-894x(01)00249-9
11363005 60526 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 453 7 2 3 5.5 COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL175634 60526 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 453 7 2 3 5.5 COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44281673 110412 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 572 10 3 5 5.6 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@H](C(=O)Nc1ccccc1)c1ccccc1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL32410 110412 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 572 10 3 5 5.6 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@H](C(=O)Nc1ccccc1)c1ccccc1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
76331527 103418 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 486 6 1 3 6.6 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1OC1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084575 103418 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 486 6 1 3 6.6 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1OC1CCCCC1 10.1016/j.bmc.2008.08.006
71458677 81501 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 423 7 3 4 3.7 O=C(Nc1ccc(OCCO)cc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2159868 81501 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 423 7 3 4 3.7 O=C(Nc1ccc(OCCO)cc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
76316939 103422 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 513 5 1 3 5.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084579 103422 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 513 5 1 3 5.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmc.2008.08.006
45270978 198970 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 489 5 1 3 4.7 O=C(C=C1CCN(C(=O)c2cccc(F)c2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL563536 198970 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 489 5 1 3 4.7 O=C(C=C1CCN(C(=O)c2cccc(F)c2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44282048 111699 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 520 9 3 5 4.2 COc1ccccc1NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL32852 111699 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 520 9 3 5 4.2 COc1ccccc1NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
44282385 100137 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 562 7 1 6 6.1 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)c1nc(C(=O)N2CCc3ccccc3C2)cs1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL287320 100137 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 562 7 1 6 6.1 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)c1nc(C(=O)N2CCc3ccccc3C2)cs1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
76327878 103414 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccncc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084571 103414 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccncc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
70686358 76173 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 578 5 2 3 6.1 O=C(Nc1ccccc1Br)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2057763 76173 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 578 5 2 3 6.1 O=C(Nc1ccccc1Br)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
70682102 76176 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 518 5 2 3 5.4 O=C(Nc1ccccc1F)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2057766 76176 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 518 5 2 3 5.4 O=C(Nc1ccccc1F)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
2729098 80526 None 0 Human Functional pIC50 = 5.9 5.9 -11 2
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL214726 80526 None 0 Human Functional pIC50 = 5.9 5.9 -11 2
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmc.2007.10.003
76309741 103423 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ncccc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084580 103423 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ncccc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
44399469 166221 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory concentration against BaF3 cell line expressed recombinant human CCR3 using the LDH assayInhibitory concentration against BaF3 cell line expressed recombinant human CCR3 using the LDH assay
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL426089 166221 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory concentration against BaF3 cell line expressed recombinant human CCR3 using the LDH assayInhibitory concentration against BaF3 cell line expressed recombinant human CCR3 using the LDH assay
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
71449677 81496 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 448 5 2 4 2.3 CS(=O)(=O)N1CCC(NC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmcl.2012.09.035
CHEMBL2159863 81496 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 448 5 2 4 2.3 CS(=O)(=O)N1CCC(NC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmcl.2012.09.035
45271843 198826 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1ccc(O)c(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c1 10.1016/j.bmc.2009.06.066
CHEMBL562574 198826 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1ccc(O)c(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c1 10.1016/j.bmc.2009.06.066
45267629 198806 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 424 5 1 2 5.7 O=C(N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL562475 198806 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 424 5 1 2 5.7 O=C(N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
23509697 196586 None 0 Human Functional pIC50 = 6.9 6.9 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 440 6 2 4 3.6 COc1cccc(NC(=O)N2CCNC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL54273 196586 None 0 Human Functional pIC50 = 6.9 6.9 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 440 6 2 4 3.6 COc1cccc(NC(=O)N2CCNC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44282006 123714 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 525 10 3 5 4.3 COc1ccc(C[C@H](NC(=O)c2cccc3ccccc23)C(=O)N[C@@H](C)C(=O)Nc2ccccc2OC)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL36195 123714 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 525 10 3 5 4.3 COc1ccc(C[C@H](NC(=O)c2cccc3ccccc23)C(=O)N[C@@H](C)C(=O)Nc2ccccc2OC)cc1 10.1016/s0960-894x(01)00249-9
44440402 93970 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of calcium fluxAntagonist activity at human CCR3 receptor assessed as inhibition of calcium flux
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL248179 93970 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of calcium fluxAntagonist activity at human CCR3 receptor assessed as inhibition of calcium flux
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440402 93970 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of eotaxin-induced eosinophil shape changeAntagonist activity at human CCR3 receptor assessed as inhibition of eotaxin-induced eosinophil shape change
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL248179 93970 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of eotaxin-induced eosinophil shape changeAntagonist activity at human CCR3 receptor assessed as inhibition of eotaxin-induced eosinophil shape change
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
45270977 197607 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 409 4 1 3 3.2 CC(=O)N1CCC(=CC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmc.2009.06.066
CHEMBL550255 197607 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 409 4 1 3 3.2 CC(=O)N1CCC(=CC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmc.2009.06.066
70682100 76167 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 568 4 1 3 5.9 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCN(C(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057757 76167 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 568 4 1 3 5.9 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCN(C(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2012.06.042
11430170 123900 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 423 6 2 2 5.5 O=C(Nc1ccccc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL362466 123900 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 423 6 2 2 5.5 O=C(Nc1ccccc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
45271911 197304 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL549514 197304 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44452250 96287 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 362 4 1 2 4.8 O=C(Nc1ccccc1)C1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
CHEMBL260900 96287 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 362 4 1 2 4.8 O=C(Nc1ccccc1)C1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
44281793 100168 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 414 7 1 5 4.7 CCn1ccnc1[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL287538 100168 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 414 7 1 5 4.7 CCn1ccnc1[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
70688459 76166 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 568 5 1 3 6.7 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(Cc2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057756 76166 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 568 5 1 3 6.7 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(Cc2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2012.06.042
44281891 125775 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 474 8 2 6 4.7 CCNC(=O)c1csc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
CHEMBL36473 125775 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 474 8 2 6 4.7 CCNC(=O)c1csc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
44281612 109681 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 510 9 3 5 4.2 C[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00249-9
CHEMBL32224 109681 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 510 9 3 5 4.2 C[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00249-9
10194663 81531 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 423 7 3 4 3.7 O=C(Nc1cccc(OCCO)c1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160104 81531 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 423 7 3 4 3.7 O=C(Nc1cccc(OCCO)c1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
70692659 76112 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 499 7 1 3 5.5 O=C(NCCCN1CCC(C(c2ccccc2)c2ccccc2)CC1)N1CCc2cc(F)ccc2C1=O 10.1016/j.bmcl.2012.06.042
CHEMBL2057490 76112 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 499 7 1 3 5.5 O=C(NCCCN1CCC(C(c2ccccc2)c2ccccc2)CC1)N1CCc2cc(F)ccc2C1=O 10.1016/j.bmcl.2012.06.042
11409583 69804 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 507 8 2 4 5.9 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1021/jm049530m
CHEMBL193575 69804 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 507 8 2 4 5.9 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1021/jm049530m
11454941 71166 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 505 7 2 6 4.7 Cc1nnnn1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL195555 71166 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 505 7 2 6 4.7 Cc1nnnn1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11328714 79029 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113074 79029 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11488078 79032 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113077 79032 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11169258 140984 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 587 8 2 10 3.8 Cn1nnnc1-c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1021/jm049530m
CHEMBL382108 140984 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 587 8 2 10 3.8 Cn1nnnc1-c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1021/jm049530m
44401328 71120 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL195348 71120 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
71460525 81538 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 526 6 3 5 3.4 O=C(NC1CCN(S(=O)(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160111 81538 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 526 6 3 5 3.4 O=C(NC1CCN(S(=O)(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
44290039 178907 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL46905 178907 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11953409 94269 None 0 Human Functional pIC50 = 8.6 8.6 7 4
Antagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assayAntagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assay
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249854 94269 None 0 Human Functional pIC50 = 8.6 8.6 7 4
Antagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assayAntagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assay
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44447144 168875 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 483 11 3 7 3.0 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(C)CCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL437396 168875 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 483 11 3 7 3.0 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(C)CCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
10474776 113721 None 32 Human Functional pIC50 = 7.7 7.7 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Functional pIC50 = 7.7 7.7 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
44281975 99683 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 491 8 2 6 3.9 C[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)OC(C)(C)C 10.1016/s0960-894x(01)00249-9
CHEMBL284166 99683 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 491 8 2 6 3.9 C[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)OC(C)(C)C 10.1016/s0960-894x(01)00249-9
44452168 95904 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 464 5 1 2 6.6 O=C(NC1C[C@@H]2CC[C@@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL258996 95904 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 464 5 1 2 6.6 O=C(NC1C[C@@H]2CC[C@@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2007.10.003
24882359 193156 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 464 5 1 2 6.6 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2008.08.006
CHEMBL522295 193156 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 464 5 1 2 6.6 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2008.08.006
70696744 76113 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 464 5 1 2 6.6 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2012.06.042
CHEMBL2057491 76113 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 464 5 1 2 6.6 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2012.06.042
24882359 193156 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 464 5 1 2 6.6 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL522295 193156 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 464 5 1 2 6.6 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
3492 692 None 0 Human Functional pIC50 = 7.7 7.7 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
9868459 692 None 0 Human Functional pIC50 = 7.7 7.7 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
CHEMBL50593 692 None 0 Human Functional pIC50 = 7.7 7.7 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
11272103 124442 None 0 Mouse Functional pIC50 = 7.7 7.7 -1995 8
Inhibition of eotaxin-induced chemotaxis of mouse eosinophilsInhibition of eotaxin-induced chemotaxis of mouse eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Mouse Functional pIC50 = 7.7 7.7 -1995 8
Inhibition of eotaxin-induced chemotaxis of mouse eosinophilsInhibition of eotaxin-induced chemotaxis of mouse eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
22393339 186842 None 0 Human Functional pIC50 = 6.7 6.7 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 410 7 2 3 4.7 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(Cl)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL48873 186842 None 0 Human Functional pIC50 = 6.7 6.7 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 410 7 2 3 4.7 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(Cl)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
23509693 191602 None 0 Human Functional pIC50 = 6.7 6.7 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 540 6 1 5 5.2 COc1cccc(NC(=O)N2CCN(C(=O)OC(C)(C)C)C(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51937 191602 None 0 Human Functional pIC50 = 6.7 6.7 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 540 6 1 5 5.2 COc1cccc(NC(=O)N2CCN(C(=O)OC(C)(C)C)C(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
71462227 81535 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 466 4 0 3 6.6 O=C1OC2(CCN(Cc3ccc4cc(F)ccc4c3)CC2)c2ccccc2N1Cc1ccccc1 10.1016/j.bmcl.2012.09.035
CHEMBL2160108 81535 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 466 4 0 3 6.6 O=C1OC2(CCN(Cc3ccc4cc(F)ccc4c3)CC2)c2ccccc2N1Cc1ccccc1 10.1016/j.bmcl.2012.09.035
45270135 197723 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 441 5 2 4 3.6 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)NS(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL551205 197723 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 441 5 2 4 3.6 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)NS(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.06.066
45268444 198474 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 458 6 1 3 5.6 O=C(C=C1CCC(Oc2ccccc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL560135 198474 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 458 6 1 3 5.6 O=C(C=C1CCC(Oc2ccccc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44282030 111695 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 461 8 1 7 3.5 CCOC(=O)C1COC([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)=N1 10.1016/s0960-894x(01)00249-9
CHEMBL32850 111695 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 461 8 1 7 3.5 CCOC(=O)C1COC([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)=N1 10.1016/s0960-894x(01)00249-9
76320670 103417 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 454 5 1 4 5.1 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-n1ccnc1 10.1016/j.bmc.2008.08.006
CHEMBL3084574 103417 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 454 5 1 4 5.1 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-n1ccnc1 10.1016/j.bmc.2008.08.006
45270980 197632 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 489 5 1 3 4.7 O=C(C=C1CCN(C(=O)c2ccc(F)cc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL550464 197632 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 489 5 1 3 4.7 O=C(C=C1CCN(C(=O)c2ccc(F)cc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44447361 95006 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 453 9 4 8 1.8 C[C@@H]([C@@H](O)c1ccccc1)N(C)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254503 95006 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophilAntagonist activity at human CCR3 receptor assessed as inhibition of chemotaxis in eosinophil
ChEMBL 453 9 4 8 1.8 C[C@@H]([C@@H](O)c1ccccc1)N(C)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
23509695 189848 None 0 Human Functional pIC50 = 6.7 6.7 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCOC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51584 189848 None 0 Human Functional pIC50 = 6.7 6.7 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCOC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
76331526 103409 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 453 5 1 3 5.7 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-n1cccc1 10.1016/j.bmc.2008.08.006
CHEMBL3084566 103409 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 453 5 1 3 5.7 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-n1cccc1 10.1016/j.bmc.2008.08.006
76327880 103421 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 485 5 1 3 5.1 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084578 103421 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 485 5 1 3 5.1 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCCC1 10.1016/j.bmc.2008.08.006
44281943 100287 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 387 6 1 5 4.5 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)c1cnco1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL288554 100287 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 387 6 1 5 4.5 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)c1cnco1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
71453334 81523 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 407 6 2 3 4.5 COCc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160097 81523 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 407 6 2 3 4.5 COCc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
76316938 103410 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 499 5 1 3 5.5 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084567 103410 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 499 5 1 3 5.5 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
44512619 103424 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 516 5 1 4 4.2 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1cc[n+]([O-])cc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084581 103424 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 516 5 1 4 4.2 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1cc[n+]([O-])cc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
45270199 198874 None 0 Human Functional pIC50 = 7.6 7.6 47 2
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 516 5 1 4 4.2 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1cc[n+]([O-])cc1C(=O)N1CCCCC1 10.1016/j.bmc.2009.06.066
CHEMBL562897 198874 None 0 Human Functional pIC50 = 7.6 7.6 47 2
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 516 5 1 4 4.2 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1cc[n+]([O-])cc1C(=O)N1CCCCC1 10.1016/j.bmc.2009.06.066
44401561 124188 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL363373 124188 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
45271882 197715 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 366 4 1 2 4.1 O=C(N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccc(F)cc1 10.1016/j.bmc.2009.06.066
CHEMBL551134 197715 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 366 4 1 2 4.1 O=C(N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccc(F)cc1 10.1016/j.bmc.2009.06.066
71455029 81502 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 464 7 2 4 3.8 CN(C)C(=O)COc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2159869 81502 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 464 7 2 4 3.8 CN(C)C(=O)COc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
70696753 76172 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 500 5 2 3 5.3 O=C(Nc1ccccc1)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2057762 76172 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 500 5 2 3 5.3 O=C(Nc1ccccc1)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
44452009 96000 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 392 5 1 3 4.4 COc1ccc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)cc1 10.1016/j.bmc.2007.10.003
CHEMBL259409 96000 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 392 5 1 3 4.4 COc1ccc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)cc1 10.1016/j.bmc.2007.10.003
10474776 113721 None 32 Human Functional pIC50 = 7.6 7.6 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Functional pIC50 = 7.6 7.6 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
71453337 81537 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 540 5 2 5 3.8 O=C(NC1CCN(S(=O)(=O)c2ccccc2O)CC1)N1CCCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmcl.2012.09.035
CHEMBL2160110 81537 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 540 5 2 5 3.8 O=C(NC1CCN(S(=O)(=O)c2ccccc2O)CC1)N1CCCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmcl.2012.09.035
44290039 178907 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL46905 178907 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
44282005 123820 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 520 9 3 5 4.2 COc1ccc(C[C@H](NC(=O)c2cccc3ccccc23)C(=O)N[C@@H](C)C(=O)Nc2ccc(C#N)cc2)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL36223 123820 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 520 9 3 5 4.2 COc1ccc(C[C@H](NC(=O)c2cccc3ccccc23)C(=O)N[C@@H](C)C(=O)Nc2ccc(C#N)cc2)cc1 10.1016/s0960-894x(01)00249-9
45269291 198896 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 427 5 2 4 3.2 O=C(N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)NS(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL563019 198896 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 427 5 2 4 3.2 O=C(N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)NS(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.06.066
45269385 198936 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 424 5 1 2 5.7 O=C(N[C@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL563319 198936 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 424 5 1 2 5.7 O=C(N[C@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
44281668 110485 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 500 8 3 4 4.4 C[C@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1cccnc1 10.1016/s0960-894x(01)00249-9
CHEMBL32451 110485 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 500 8 3 4 4.4 C[C@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1cccnc1 10.1016/s0960-894x(01)00249-9
44452168 95904 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 464 5 1 2 6.6 O=C(NC1C[C@@H]2CC[C@@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL258996 95904 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 464 5 1 2 6.6 O=C(NC1C[C@@H]2CC[C@@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2007.10.003
76320671 103419 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 471 5 1 3 5.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084576 103419 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 471 5 1 3 5.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1N1CCCCC1 10.1016/j.bmc.2008.08.006
71456839 81527 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 467 10 3 5 3.8 O=C(Nc1ccccc1OCCOCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160100 81527 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 467 10 3 5 3.8 O=C(Nc1ccccc1OCCOCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
44452220 161370 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 452 5 1 2 6.4 CC1(NC(=O)c2ccccc2-c2ccccc2)CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
CHEMBL412072 161370 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 452 5 1 2 6.4 CC1(NC(=O)c2ccccc2-c2ccccc2)CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
76313428 103407 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 465 5 1 3 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1cccnc1 10.1016/j.bmc.2008.08.006
CHEMBL3084564 103407 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 465 5 1 3 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1cccnc1 10.1016/j.bmc.2008.08.006
70688469 76214 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 534 5 2 3 5.9 O=C(Nc1ccccc1Cl)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2058070 76214 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 534 5 2 3 5.9 O=C(Nc1ccccc1Cl)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
44452119 96407 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1F 10.1016/j.bmc.2007.10.003
CHEMBL261574 96407 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1F 10.1016/j.bmc.2007.10.003
44281859 109881 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 463 9 2 6 3.2 CCOC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL32334 109881 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 463 9 2 6 3.2 CCOC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
44289926 177664 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 453 9 2 4 4.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL46404 177664 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 453 9 2 4 4.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
44289927 168430 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL43423 168430 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
45268462 198671 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c(O)c1 10.1016/j.bmc.2009.06.066
CHEMBL561535 198671 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c(O)c1 10.1016/j.bmc.2009.06.066
45269302 198572 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 531 7 1 5 4.5 COc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)cc1OC 10.1016/j.bmc.2009.06.066
CHEMBL560995 198572 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 531 7 1 5 4.5 COc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)cc1OC 10.1016/j.bmc.2009.06.066
70688470 76217 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 542 6 2 3 6.4 CC(C)c1ccccc1NC(=O)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2058073 76217 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 542 6 2 3 6.4 CC(C)c1ccccc1NC(=O)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
9892753 16507 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 516 8 3 4 5.5 CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm049530m
CHEMBL123611 16507 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 516 8 3 4 5.5 CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm049530m
44281667 115725 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 524 10 3 5 3.9 CC(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00249-9
CHEMBL33537 115725 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 524 10 3 5 3.9 CC(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00249-9
45273705 198254 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 376 5 1 2 4.3 O=C(Cc1ccccc1)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2009.06.066
CHEMBL557936 198254 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 376 5 1 2 4.3 O=C(Cc1ccccc1)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2009.06.066
10050884 154742 None 15 Mouse Functional pIC50 = 7.5 7.5 -204 3
Antagonist activity at CCR3 receptor in mouse eosinophil assessed as as inhibition of chemotaxisAntagonist activity at CCR3 receptor in mouse eosinophil assessed as as inhibition of chemotaxis
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL399495 154742 None 15 Mouse Functional pIC50 = 7.5 7.5 -204 3
Antagonist activity at CCR3 receptor in mouse eosinophil assessed as as inhibition of chemotaxisAntagonist activity at CCR3 receptor in mouse eosinophil assessed as as inhibition of chemotaxis
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
70684230 76216 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 530 6 2 4 5.3 COc1ccccc1NC(=O)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2058072 76216 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 530 6 2 4 5.3 COc1ccccc1NC(=O)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
70682099 76162 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 532 4 1 3 5.2 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057752 76162 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 532 4 1 3 5.2 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.06.042
10474776 113721 None 32 Human Functional pIC50 = 7.5 7.5 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Functional pIC50 = 7.5 7.5 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
45268519 198729 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 409 5 0 2 6.4 O=C(c1ccccc1-c1ccccc1)C1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL561941 198729 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 409 5 0 2 6.4 O=C(c1ccccc1-c1ccccc1)C1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44281966 99866 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 403 6 1 5 4.9 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)c1nccs1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL285444 99866 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 403 6 1 5 4.9 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)c1nccs1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
44452361 96561 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 338 5 1 2 3.7 O=C(NC1CCN(C/C=C/c2ccc(F)cc2)CC1)c1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL262588 96561 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 338 5 1 2 3.7 O=C(NC1CCN(C/C=C/c2ccc(F)cc2)CC1)c1ccccc1 10.1016/j.bmc.2007.10.003
10474776 113721 None 32 Human Functional pIC50 = 7.5 7.5 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Functional pIC50 = 7.5 7.5 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11442439 124124 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 455 6 2 2 5.9 Cc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1F 10.1021/jm049530m
CHEMBL363166 124124 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 455 6 2 2 5.9 Cc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1F 10.1021/jm049530m
44386406 62507 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 461 9 2 6 3.3 C=C(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)OCC 10.1016/s0960-894x(01)00249-9
CHEMBL178019 62507 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 461 9 2 6 3.3 C=C(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)OCC 10.1016/s0960-894x(01)00249-9
6918497 113493 None 1 Mouse Functional pIC50 = 6.5 6.5 -213 4
Inhibitory activity against I-Eotaxin induced [Ca2+] response in mouse CCR3 receptorInhibitory activity against I-Eotaxin induced [Ca2+] response in mouse CCR3 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Functional pIC50 = 6.5 6.5 -213 4
Inhibitory activity against I-Eotaxin induced [Ca2+] response in mouse CCR3 receptorInhibitory activity against I-Eotaxin induced [Ca2+] response in mouse CCR3 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Functional pIC50 = 6.5 6.5 -213 4
Inhibitory activity against I-Eotaxin induced [Ca2+] response in mouse CCR3 receptorInhibitory activity against I-Eotaxin induced [Ca2+] response in mouse CCR3 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
44452044 156178 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 392 5 1 3 4.4 COc1cccc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmc.2007.10.003
CHEMBL406296 156178 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 392 5 1 3 4.4 COc1cccc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmc.2007.10.003
70690518 76158 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 555 4 1 4 5.0 CN1CN(c2ccccc2)C2(CCN(C(=O)NC3C[C@H]4CC[C@H](C3)N4Cc3ccc4cc(F)ccc4c3)CC2)C1=O 10.1016/j.bmcl.2012.06.042
CHEMBL2057748 76158 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 555 4 1 4 5.0 CN1CN(c2ccccc2)C2(CCN(C(=O)NC3C[C@H]4CC[C@H](C3)N4Cc3ccc4cc(F)ccc4c3)CC2)C1=O 10.1016/j.bmcl.2012.06.042
10474776 113721 None 32 Human Functional pIC50 = 7.4 7.4 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using [Ca2+] mobilization assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using [Ca2+] mobilization assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Functional pIC50 = 7.4 7.4 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using [Ca2+] mobilization assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using [Ca2+] mobilization assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
44451928 159256 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 438 5 1 2 6.0 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL409830 159256 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 438 5 1 2 6.0 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2007.10.003
44451928 159256 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 438 5 1 2 6.0 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL409830 159256 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 438 5 1 2 6.0 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
45268458 199199 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1cccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c1O 10.1016/j.bmc.2009.06.066
CHEMBL565165 199199 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1cccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c1O 10.1016/j.bmc.2009.06.066
71460524 81536 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 474 5 1 3 4.9 O=C(NC1CCN(Cc2ccccc2)CC1)N1CCCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmcl.2012.09.035
CHEMBL2160109 81536 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 474 5 1 3 4.9 O=C(NC1CCN(Cc2ccccc2)CC1)N1CCCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmcl.2012.09.035
70686357 76163 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 529 4 2 4 4.6 Nc1ccc(C(=O)N2CCCN(C(=O)NC3C[C@H]4CC[C@H](C3)N4Cc3ccc4cc(F)ccc4c3)CC2)cc1 10.1016/j.bmcl.2012.06.042
CHEMBL2057753 76163 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 529 4 2 4 4.6 Nc1ccc(C(=O)N2CCCN(C(=O)NC3C[C@H]4CC[C@H](C3)N4Cc3ccc4cc(F)ccc4c3)CC2)cc1 10.1016/j.bmcl.2012.06.042
44282280 120457 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 463 9 2 6 3.2 CCOC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL35341 120457 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 463 9 2 6 3.2 CCOC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
11329244 71140 None 6 Human Functional pIC50 = 8.4 8.4 20 7
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71140 None 6 Human Functional pIC50 = 8.4 8.4 20 7
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11340670 127301 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 483 7 2 3 5.8 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)ccc1F 10.1021/jm049530m
CHEMBL365820 127301 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 483 7 2 3 5.8 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)ccc1F 10.1021/jm049530m
11397114 133537 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2cn[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL3706810 133537 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2cn[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44401123 136365 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 516 7 2 5 4.9 N#CC1=CC(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)CC=C1n1cccn1 10.1021/jm049530m
CHEMBL373347 136365 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 516 7 2 5 4.9 N#CC1=CC(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)CC=C1n1cccn1 10.1021/jm049530m
9847583 198922 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 471 5 1 3 4.5 O=C(C=C1CCN(C(=O)c2ccccc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL563189 198922 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 471 5 1 3 4.5 O=C(C=C1CCN(C(=O)c2ccccc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
45273624 198123 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 489 5 1 3 4.7 O=C(C=C1CCN(C(=O)c2ccccc2F)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL556500 198123 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 489 5 1 3 4.7 O=C(C=C1CCN(C(=O)c2ccccc2F)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
70696765 76215 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 545 6 2 5 5.2 O=C(Nc1ccccc1[N+](=O)[O-])[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2058071 76215 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 545 6 2 5 5.2 O=C(Nc1ccccc1[N+](=O)[O-])[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
25024651 116100 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of CCR3 in human eosinophil assessed as inhibition of eotaxin-induced Ca2+ influxInhibition of CCR3 in human eosinophil assessed as inhibition of eotaxin-induced Ca2+ influx
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355956 116100 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of CCR3 in human eosinophil assessed as inhibition of eotaxin-induced Ca2+ influxInhibition of CCR3 in human eosinophil assessed as inhibition of eotaxin-induced Ca2+ influx
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
44281706 111621 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 496 9 3 5 3.8 O=C(CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)Nc1ccccc1 10.1016/s0960-894x(01)00249-9
CHEMBL32806 111621 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 496 9 3 5 3.8 O=C(CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)Nc1ccccc1 10.1016/s0960-894x(01)00249-9
11227406 94398 None 2 Mouse Functional pIC50 = 7.4 7.4 -107 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL250689 94398 None 2 Mouse Functional pIC50 = 7.4 7.4 -107 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
71460504 81497 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 369 4 2 2 4.2 O=C(NC1CCCCC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2159864 81497 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 369 4 2 2 4.2 O=C(NC1CCCCC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
11227406 94398 None 2 Mouse Functional pIC50 = 7.4 7.4 -107 4
Inhibition of eotaxin-induced chemotaxis of mouse eosinophilsInhibition of eotaxin-induced chemotaxis of mouse eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL250689 94398 None 2 Mouse Functional pIC50 = 7.4 7.4 -107 4
Inhibition of eotaxin-induced chemotaxis of mouse eosinophilsInhibition of eotaxin-induced chemotaxis of mouse eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
71456816 81499 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 407 6 3 3 3.9 O=C(Nc1ccccc1CCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2159866 81499 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 407 6 3 3 3.9 O=C(Nc1ccccc1CCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
71455044 81532 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 450 8 2 4 4.3 CN(C)CCOc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160105 81532 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 450 8 2 4 4.3 CN(C)CCOc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
71453336 81533 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 436 7 3 4 3.2 NC(=O)COc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160106 81533 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 436 7 3 4 3.2 NC(=O)COc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
76327879 103420 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 527 6 1 3 6.3 CN(C(=O)c1ccccc1C(=O)N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)C1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084577 103420 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 527 6 1 3 6.3 CN(C(=O)c1ccccc1C(=O)N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)C1CCCCC1 10.1016/j.bmc.2008.08.006
70682098 76160 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 545 4 2 4 5.3 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057750 76160 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 545 4 2 4 5.3 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1 10.1016/j.bmcl.2012.06.042
70682101 76168 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 530 4 2 4 4.7 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2ccc(O)cc2)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057758 76168 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 530 4 2 4 4.7 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2ccc(O)cc2)CC1 10.1016/j.bmcl.2012.06.042
44281852 99736 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 511 8 3 3 5.1 Cc1ccc(C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](C)C(=O)Nc2ccc(Cl)cc2)c(C)c1 10.1016/s0960-894x(01)00249-9
CHEMBL284531 99736 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 511 8 3 3 5.1 Cc1ccc(C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](C)C(=O)Nc2ccc(Cl)cc2)c(C)c1 10.1016/s0960-894x(01)00249-9
44281944 121858 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 529 9 3 4 5.0 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL35896 121858 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 529 9 3 4 5.0 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
70692666 76170 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 554 5 1 3 5.5 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)C2(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057760 76170 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 554 5 1 3 5.5 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)C2(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2012.06.042
45273639 198881 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1cccc(O)c1C(=O)N1CCC(=CC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmc.2009.06.066
CHEMBL562922 198881 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 517 6 2 5 4.2 COc1cccc(O)c1C(=O)N1CCC(=CC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmc.2009.06.066
44452172 95905 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 378 4 1 3 5.2 O=C(Nc1ccccc1)OC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
CHEMBL258997 95905 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 378 4 1 3 5.2 O=C(Nc1ccccc1)OC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
76324312 103411 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 514 5 1 4 4.3 CN1CCN(C(=O)c2ccccc2C(=O)N[C@H]2C[C@@H]3CC[C@H](C2)N3Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2008.08.006
CHEMBL3084568 103411 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 514 5 1 4 4.3 CN1CCN(C(=O)c2ccccc2C(=O)N[C@H]2C[C@@H]3CC[C@H](C2)N3Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2008.08.006
10474776 113721 None 32 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL33227 113721 None 32 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
9957612 163357 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 499 8 3 3 5.0 C[C@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00249-9
CHEMBL418588 163357 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 499 8 3 3 5.0 C[C@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00249-9
45273632 198159 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2cccc(O)c2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL556916 198159 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2cccc(O)c2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44455847 155536 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 501 9 2 6 4.7 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL403839 155536 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 501 9 2 6 4.7 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
45272697 198077 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 6 1 4 4.5 COc1ccccc1C(=O)N1CCC(=CC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmc.2009.06.066
CHEMBL556227 198077 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 6 1 4 4.5 COc1ccccc1C(=O)N1CCC(=CC(=O)N[C@@H]2CCN(Cc3ccc4cc(F)ccc4c3)C2)CC1 10.1016/j.bmc.2009.06.066
45273698 198882 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccc(O)cc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL562923 198882 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccc(O)cc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
45273689 198182 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 6 1 4 4.5 COc1cccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c1 10.1016/j.bmc.2009.06.066
CHEMBL557118 198182 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 501 6 1 4 4.5 COc1cccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)c1 10.1016/j.bmc.2009.06.066
71455028 81498 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 363 4 2 2 4.4 O=C(Nc1ccccc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2159865 81498 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 363 4 2 2 4.4 O=C(Nc1ccccc1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
71453335 81530 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 437 8 3 4 4.1 O=C(Nc1ccccc1OCCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160103 81530 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 437 8 3 4 4.1 O=C(Nc1ccccc1OCCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
11179592 69614 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 501 6 2 2 6.2 O=C(Nc1ccc(Br)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL193442 69614 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 501 6 2 2 6.2 O=C(Nc1ccc(Br)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11316656 70286 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 441 6 2 2 5.6 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL194141 70286 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 441 6 2 2 5.6 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44281755 99741 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 502 9 3 6 3.8 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](Cc2cscn2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL284576 99741 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 502 9 3 6 3.8 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](Cc2cscn2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
44281999 121923 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 459 8 1 7 4.6 CCOC(=O)c1coc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
CHEMBL35900 121923 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 459 8 1 7 4.6 CCOC(=O)c1coc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
71462226 81524 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 421 7 3 3 4.3 O=C(Nc1ccccc1CCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160098 81524 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 421 7 3 3 4.3 O=C(Nc1ccccc1CCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
70694702 76165 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 548 4 2 4 4.9 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2c(O)cccc2F)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057755 76165 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 548 4 2 4 4.9 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2c(O)cccc2F)CC1 10.1016/j.bmcl.2012.06.042
70690519 76159 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 527 4 2 4 5.2 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057749 76159 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 527 4 2 4 5.2 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.06.042
10474776 113721 None 32 Human Functional pIC50 = 7.3 7.3 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Functional pIC50 = 7.3 7.3 - 1
Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assayAgonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
45271905 197268 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 438 5 1 2 6.0 O=C(NC1CCCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
CHEMBL549302 197268 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 438 5 1 2 6.0 O=C(NC1CCCN(Cc2ccc3cc(F)ccc3c2)C1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2009.06.066
70690520 76171 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 550 5 1 4 4.6 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057761 76171 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 550 5 1 4 4.6 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.06.042
9952288 110567 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 389 6 1 5 3.5 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C1=NCCO1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL32493 110567 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 389 6 1 5 3.5 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C1=NCCO1)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
76324313 103416 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 465 5 1 3 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccn1 10.1016/j.bmc.2008.08.006
CHEMBL3084573 103416 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 465 5 1 3 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccn1 10.1016/j.bmc.2008.08.006
70690517 76157 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 541 4 2 4 4.6 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2012.06.042
CHEMBL2057747 76157 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 541 4 2 4 4.6 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2012.06.042
45268467 198698 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 505 5 2 4 4.4 O=C(C=C1CCN(C(=O)c2ccc(F)cc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL561740 198698 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 505 5 2 4 4.4 O=C(C=C1CCN(C(=O)c2ccc(F)cc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
6918497 113493 None 1 Human Functional pIC50 = 8.2 8.2 1 4
Inhibitory activity against I-Eotaxin induced [Ca2+] response in human CCR3 receptorInhibitory activity against I-Eotaxin induced [Ca2+] response in human CCR3 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Human Functional pIC50 = 8.2 8.2 1 4
Inhibitory activity against I-Eotaxin induced [Ca2+] response in human CCR3 receptorInhibitory activity against I-Eotaxin induced [Ca2+] response in human CCR3 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Human Functional pIC50 = 8.2 8.2 1 4
Inhibitory activity against I-Eotaxin induced [Ca2+] response in human CCR3 receptorInhibitory activity against I-Eotaxin induced [Ca2+] response in human CCR3 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
44455872 155605 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL404202 155605 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxisAntagonist activity at human CCR3 receptor in human eosinophil assessed as inhibition of eotaxin-induced chemotaxis
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
44281987 99702 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 542 9 3 4 5.4 C[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL284313 99702 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 542 9 3 4 5.4 C[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00249-9
44281794 168114 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 524 9 2 5 4.3 C[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)N(C)c1ccccc1 10.1016/s0960-894x(01)00249-9
CHEMBL432088 168114 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 524 9 2 5 4.3 C[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)N(C)c1ccccc1 10.1016/s0960-894x(01)00249-9
44452304 157937 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 348 5 1 2 4.7 Fc1ccc2cc(CN3CCC(NCc4ccccc4)CC3)ccc2c1 10.1016/j.bmc.2007.10.003
CHEMBL408368 157937 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 348 5 1 2 4.7 Fc1ccc2cc(CN3CCC(NCc4ccccc4)CC3)ccc2c1 10.1016/j.bmc.2007.10.003
71449695 81534 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 416 5 0 2 5.0 O=C1N(CCc2ccccc2)CCC12CCN(Cc1ccc3cc(F)ccc3c1)CC2 10.1016/j.bmcl.2012.09.035
CHEMBL2160107 81534 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 416 5 0 2 5.0 O=C1N(CCc2ccccc2)CCC12CCN(Cc1ccc3cc(F)ccc3c1)CC2 10.1016/j.bmcl.2012.09.035
9826988 76111 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 492 7 0 7 4.2 Cc1nnc2n(CCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)c(=O)c3ccccc3n12 10.1016/j.bmcl.2012.06.042
CHEMBL2057489 76111 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 492 7 0 7 4.2 Cc1nnc2n(CCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)c(=O)c3ccccc3n12 10.1016/j.bmcl.2012.06.042
76320667 103406 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 465 5 1 3 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccncc1 10.1016/j.bmc.2008.08.006
CHEMBL3084563 103406 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 465 5 1 3 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccncc1 10.1016/j.bmc.2008.08.006
24882359 193156 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 464 5 1 2 6.6 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2008.08.006
CHEMBL522295 193156 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 464 5 1 2 6.6 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1ccccc1 10.1016/j.bmc.2008.08.006
70694701 76164 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 582 4 1 3 6.3 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057754 76164 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 582 4 1 3 6.3 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2012.06.042
70696752 76169 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 530 4 2 4 4.7 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2ccccc2O)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057759 76169 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 530 4 2 4 4.7 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCCN(C(=O)c2ccccc2O)CC1 10.1016/j.bmcl.2012.06.042
44452086 157979 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2007.10.003
CHEMBL408407 157979 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2007.10.003
44452086 157979 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2009.06.066
CHEMBL408407 157979 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2009.06.066
44281775 115627 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 524 9 2 5 4.6 C[C@@H](C(=O)Nc1ccccc1)N(C)C(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL33534 115627 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 524 9 2 5 4.6 C[C@@H](C(=O)Nc1ccccc1)N(C)C(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
44281951 120291 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 475 8 1 7 5.1 CCOC(=O)c1csc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
CHEMBL35217 120291 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 475 8 1 7 5.1 CCOC(=O)c1csc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
44281686 112089 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 462 9 3 5 2.7 CCNC(=O)C(C)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
CHEMBL32895 112089 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 462 9 3 5 2.7 CCNC(=O)C(C)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00249-9
44452120 156320 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1cccc(F)c1 10.1016/j.bmc.2007.10.003
CHEMBL406468 156320 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1cccc(F)c1 10.1016/j.bmc.2007.10.003
76313429 103412 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 501 5 1 4 4.4 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCOCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084569 103412 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 501 5 1 4 4.4 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1C(=O)N1CCOCC1 10.1016/j.bmc.2008.08.006
11953409 94269 None 0 Mouse Functional pIC50 = 8.2 8.2 -7 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophils
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249854 94269 None 0 Mouse Functional pIC50 = 8.2 8.2 -7 4
Antagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophilsAntagonist activity at CCR3 assessed as eotaxin-induced chemotaxis in BALB/c mouse eosinophils
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
45269320 199048 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 521 5 2 4 4.9 O=C(C=C1CCN(C(=O)c2ccc(Cl)cc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL564022 199048 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 521 5 2 4 4.9 O=C(C=C1CCN(C(=O)c2ccc(Cl)cc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44281774 116731 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 501 9 3 4 5.1 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL33708 116731 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 501 9 3 4 5.1 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
71456840 81528 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 437 8 2 4 4.4 COCCOc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2160101 81528 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 437 8 2 4 4.4 COCCOc1ccccc1NC(=O)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
44387842 131369 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 369 5 2 3 4.2 CC(=O)c1cccc(NC(=O)NN2CCCCC2Cc2ccc(F)cc2)c1 10.1021/jm049530m
CHEMBL368683 131369 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of eotaxin-induced chemotaxis of human eosinophilsInhibition of eotaxin-induced chemotaxis of human eosinophils
ChEMBL 369 5 2 3 4.2 CC(=O)c1cccc(NC(=O)NN2CCCCC2Cc2ccc(F)cc2)c1 10.1021/jm049530m
44452083 96230 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 392 5 1 3 4.4 COc1ccccc1C(=O)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
CHEMBL260649 96230 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 392 5 1 3 4.4 COc1ccccc1C(=O)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
44281872 109414 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 522 8 2 6 6.2 O=C(Nc1ccccc1)c1csc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
CHEMBL32191 109414 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 522 8 2 6 6.2 O=C(Nc1ccccc1)c1csc([C@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)c2cccc3ccccc23)n1 10.1016/s0960-894x(01)00249-9
70684221 76156 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 461 3 1 2 5.4 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCc2cc(F)ccc2C1 10.1016/j.bmcl.2012.06.042
CHEMBL2057746 76156 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 461 3 1 2 5.4 O=C(NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)N1CCc2cc(F)ccc2C1 10.1016/j.bmcl.2012.06.042
11227406 94398 None 2 Human Functional pIC50 = 8.1 8.1 107 4
Antagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assayAntagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL250689 94398 None 2 Human Functional pIC50 = 8.1 8.1 107 4
Antagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assayAntagonist activity at CCR3 in human eosinophils assessed as eotaxin-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
70696751 76161 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 542 4 3 5 4.7 Nc1ccc2c(c1)[nH]c(=O)n2C1CCN(C(=O)NC2C[C@H]3CC[C@H](C2)N3Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmcl.2012.06.042
CHEMBL2057751 76161 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 542 4 3 5 4.7 Nc1ccc2c(c1)[nH]c(=O)n2C1CCN(C(=O)NC2C[C@H]3CC[C@H](C2)N3Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmcl.2012.06.042
11227406 94398 None 2 Human Functional pIC50 = 8.1 8.1 107 4
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL250689 94398 None 2 Human Functional pIC50 = 8.1 8.1 107 4
Inhibition of calcium mobilization in human eosinophilsInhibition of calcium mobilization in human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44512617 197794 None 0 Human Functional pIC50 = 8.1 8.1 79 2
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL551735 197794 None 0 Human Functional pIC50 = 8.1 8.1 79 2
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
22393430 168805 None 0 Human Functional pIC50 = 7.1 7.1 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL43677 168805 None 0 Human Functional pIC50 = 7.1 7.1 - 1
In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44281754 113241 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 506 8 3 5 4.4 C[C@H](NC(=O)[C@H](Cc1cscn1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccc(Cl)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL33144 113241 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 506 8 3 5 4.4 C[C@H](NC(=O)[C@H](Cc1cscn1)NC(=O)c1cccc2ccccc12)C(=O)Nc1ccc(Cl)cc1 10.1016/s0960-894x(01)00249-9
44452248 96285 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 376 4 0 2 4.7 CN(C(=O)c1ccccc1)C1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
CHEMBL260899 96285 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 376 4 0 2 4.7 CN(C(=O)c1ccccc1)C1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
44295672 188864 None 0 Human Functional pIC50 = 6.1 6.1 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 439 6 1 3 5.0 COc1cccc(NC(=O)N2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50535 188864 None 0 Human Functional pIC50 = 6.1 6.1 - 1
In vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assayIn vitro C-C chemokine receptor type 3 receptor activity of compound to inhibit eotaxin induced [Ca2+] mobilization in human eosinophil chemotaxis assay
ChEMBL 439 6 1 3 5.0 COc1cccc(NC(=O)N2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44452280 95863 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 398 5 1 3 3.9 O=S(=O)(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL258790 95863 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 398 5 1 3 3.9 O=S(=O)(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmc.2007.10.003
76313430 103415 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1cnccc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084572 103415 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1cnccc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
76320668 103408 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 471 5 1 4 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1nccs1 10.1016/j.bmc.2008.08.006
CHEMBL3084565 103408 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 471 5 1 4 6.0 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1nccs1 10.1016/j.bmc.2008.08.006
71451489 81500 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 451 9 3 4 4.5 O=C(Nc1ccccc1OCCCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
CHEMBL2159867 81500 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR3 receptorAntagonist activity at CCR3 receptor
ChEMBL 451 9 3 4 4.5 O=C(Nc1ccccc1OCCCCO)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmcl.2012.09.035
44282047 163262 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 520 9 3 5 4.2 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(C#N)cc2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
CHEMBL418041 163262 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against C-C chemokine receptor type 3Antagonist activity against C-C chemokine receptor type 3
ChEMBL 520 9 3 5 4.2 COc1ccc(NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(C#N)cc2)NC(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(01)00249-9
45273619 198934 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 485 6 1 3 4.8 O=C(/C=C/C1CCN(C(=O)c2ccccc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL563303 198934 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 485 6 1 3 4.8 O=C(/C=C/C1CCN(C(=O)c2ccccc2)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
70688460 76175 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 578 5 2 3 6.1 O=C(Nc1ccc(Br)cc1)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
CHEMBL2057765 76175 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR3Antagonist activity at human CCR3
ChEMBL 578 5 2 3 6.1 O=C(Nc1ccc(Br)cc1)[C@@H]1CCCN1C(=O)NC1C[C@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1 10.1016/j.bmcl.2012.06.042
76313415 106443 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 466 5 1 4 5.4 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1cncnc1 10.1016/j.bmc.2008.08.006
CHEMBL3084359 106443 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 466 5 1 4 5.4 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1cncnc1 10.1016/j.bmc.2008.08.006
CHEMBL3139342 106443 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 466 5 1 4 5.4 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1ccccc1-c1cncnc1 10.1016/j.bmc.2008.08.006
3536 3906 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Antagonist activity at CCR3 assessed as inhibition of CCL11-induced chemotaxis by cell based assayAntagonist activity at CCR3 assessed as inhibition of CCL11-induced chemotaxis by cell based assay
ChEMBL 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10.1021/jm300682j
44560289 3906 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Antagonist activity at CCR3 assessed as inhibition of CCL11-induced chemotaxis by cell based assayAntagonist activity at CCR3 assessed as inhibition of CCL11-induced chemotaxis by cell based assay
ChEMBL 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10.1021/jm300682j
CHEMBL1186993 3906 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Antagonist activity at CCR3 assessed as inhibition of CCL11-induced chemotaxis by cell based assayAntagonist activity at CCR3 assessed as inhibition of CCL11-induced chemotaxis by cell based assay
ChEMBL 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10.1021/jm300682j
44451983 159456 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 454 6 1 3 6.2 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1Oc1ccccc1 10.1016/j.bmc.2007.10.003
CHEMBL410041 159456 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 454 6 1 3 6.2 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1Oc1ccccc1 10.1016/j.bmc.2007.10.003
44452198 158064 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 388 5 1 2 4.8 O=C(/C=C/c1ccccc1)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
CHEMBL408486 158064 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influxAntagonist activity at CCR3 expressed in B300-19 cells assessed as inhibition of eotaxin-induced calcium influx
ChEMBL 388 5 1 2 4.8 O=C(/C=C/c1ccccc1)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2007.10.003
44452198 158064 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 388 5 1 2 4.8 O=C(/C=C/c1ccccc1)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2009.06.066
CHEMBL408486 158064 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium fluxAntagonist activity at human CCR3 expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium flux
ChEMBL 388 5 1 2 4.8 O=C(/C=C/c1ccccc1)NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1 10.1016/j.bmc.2009.06.066
76320669 103413 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1cccnc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
CHEMBL3084570 103413 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometryAntagonist activity at CCR3 receptor expressed in mouse B300-19 cells assessed as inhibition of eotaxin-induced calcium influx by spectrophotometry
ChEMBL 500 5 1 4 4.9 O=C(N[C@H]1C[C@@H]2CC[C@H](C1)N2Cc1ccc2cc(F)ccc2c1)c1cccnc1C(=O)N1CCCCC1 10.1016/j.bmc.2008.08.006
11753159 547 None 6 Human Functional pKd = 7 7.0 4 2
Antagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysisAntagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysis
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
7679 547 None 6 Human Functional pKd = 7 7.0 4 2
Antagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysisAntagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysis
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2158814 547 None 6 Human Functional pKd = 7 7.0 4 2
Antagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysisAntagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysis
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
16040671 81310 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at CCR3 in human eosinophils assessed as inhibition of CCL24-induced morphological changes by FACS flow cytometric analysisAntagonist activity at CCR3 in human eosinophils assessed as inhibition of CCL24-induced morphological changes by FACS flow cytometric analysis
ChEMBL 502 8 1 4 5.4 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158791 81310 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at CCR3 in human eosinophils assessed as inhibition of CCL24-induced morphological changes by FACS flow cytometric analysisAntagonist activity at CCR3 in human eosinophils assessed as inhibition of CCL24-induced morphological changes by FACS flow cytometric analysis
ChEMBL 502 8 1 4 5.4 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
16681693 82604 None 1 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human CCR3 assessed as inhibition of CCL11-induced calcium influx by cell based assayAntagonist activity at human CCR3 assessed as inhibition of CCL11-induced calcium influx by cell based assay
ChEMBL 487 5 1 5 3.6 Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)nn1 10.1021/jm300682j
CHEMBL2178580 82604 None 1 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human CCR3 assessed as inhibition of CCL11-induced calcium influx by cell based assayAntagonist activity at human CCR3 assessed as inhibition of CCL11-induced calcium influx by cell based assay
ChEMBL 487 5 1 5 3.6 Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)nn1 10.1021/jm300682j
44399573 68058 None 0 Human Functional pKi = 7.0 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 465 6 1 3 5.4 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)C1CCCCC1 10.1016/j.bmcl.2005.04.054
CHEMBL191418 68058 None 0 Human Functional pKi = 7.0 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 465 6 1 3 5.4 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)C1CCCCC1 10.1016/j.bmcl.2005.04.054
44399538 67557 None 0 Human Functional pKi = 6.8 6.8 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 7 1 4 5.7 O=C(NCC1CCCN(C2CCN(CCc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL189680 67557 None 0 Human Functional pKi = 6.8 6.8 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 7 1 4 5.7 O=C(NCC1CCCN(C2CCN(CCc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
44399469 166221 None 0 Human Functional pKi = 7.6 7.6 - 1
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL426089 166221 None 0 Human Functional pKi = 7.6 7.6 - 1
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
44399385 67648 None 0 Human Functional pKi = 7.5 7.5 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 498 6 2 3 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2[nH]ccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL190436 67648 None 0 Human Functional pKi = 7.5 7.5 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 498 6 2 3 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2[nH]ccc2c1 10.1016/j.bmcl.2005.04.054
11540776 69483 None 0 Human Functional pKi = 7.5 7.5 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2cccnc12 10.1016/j.bmcl.2005.04.054
CHEMBL193354 69483 None 0 Human Functional pKi = 7.5 7.5 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2cccnc12 10.1016/j.bmcl.2005.04.054
44399272 67493 None 0 Human Functional pKi = 7.5 7.5 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1nccc2ccccc12 10.1016/j.bmcl.2005.04.054
CHEMBL189206 67493 None 0 Human Functional pKi = 7.5 7.5 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1nccc2ccccc12 10.1016/j.bmcl.2005.04.054
11540776 69483 None 0 Human Functional pKi = 7.4 7.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2cccnc12 10.1016/j.bmcl.2005.04.054
CHEMBL193354 69483 None 0 Human Functional pKi = 7.4 7.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2cccnc12 10.1016/j.bmcl.2005.04.054
44399482 166123 None 0 Human Functional pKi = 7.4 7.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 498 6 2 3 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2[nH]ccc12 10.1016/j.bmcl.2005.04.054
CHEMBL425548 166123 None 0 Human Functional pKi = 7.4 7.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 498 6 2 3 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2[nH]ccc12 10.1016/j.bmcl.2005.04.054
44399443 69202 None 0 Human Functional pKi = 6.4 6.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3cc(Cl)ccc3Cl)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL192584 69202 None 0 Human Functional pKi = 6.4 6.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3cc(Cl)ccc3Cl)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
44399574 67813 None 0 Human Functional pKi = 6.4 6.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3cc(Cl)cc(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL190894 67813 None 0 Human Functional pKi = 6.4 6.4 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3cc(Cl)cc(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
44399389 127573 None 0 Human Functional pKi = 7.3 7.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 499 6 2 4 5.0 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2[nH]cnc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL366143 127573 None 0 Human Functional pKi = 7.3 7.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 499 6 2 4 5.0 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2[nH]cnc2c1 10.1016/j.bmcl.2005.04.054
44399331 127584 None 0 Human Functional pKi = 7.3 7.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 509 6 1 3 6.3 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL366199 127584 None 0 Human Functional pKi = 7.3 7.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 509 6 1 3 6.3 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.04.054
44399395 67613 None 0 Human Functional pKi = 7.3 7.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 6 1 4 6.0 CC1(N2CCCC(CNC(=O)c3ccc4ncccc4c3)C2)CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2005.04.054
CHEMBL190149 67613 None 0 Human Functional pKi = 7.3 7.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 6 1 4 6.0 CC1(N2CCCC(CNC(=O)c3ccc4ncccc4c3)C2)CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2005.04.054
44399552 67481 None 0 Human Functional pKi = 6.3 6.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 397 5 1 3 3.8 CC(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
CHEMBL189158 67481 None 0 Human Functional pKi = 6.3 6.3 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 397 5 1 3 3.8 CC(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
44399524 135588 None 0 Human Functional pKi = 7.2 7.2 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 509 6 1 3 6.3 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2005.04.054
CHEMBL372868 135588 None 0 Human Functional pKi = 7.2 7.2 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 509 6 1 3 6.3 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2005.04.054
44399368 67215 None 0 Human Functional pKi = 7.2 7.2 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 473 6 1 3 5.4 Cc1ccccc1C(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
CHEMBL187779 67215 None 0 Human Functional pKi = 7.2 7.2 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 473 6 1 3 5.4 Cc1ccccc1C(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
44399303 68113 None 0 Human Functional pKi = 8.1 8.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 6 1 4 5.9 CC1CN(Cc2ccc(Cl)c(Cl)c2)CCC1N1CCCC(CNC(=O)c2ccc3ncccc3c2)C1 10.1016/j.bmcl.2005.04.054
CHEMBL191464 68113 None 0 Human Functional pKi = 8.1 8.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 6 1 4 5.9 CC1CN(Cc2ccc(Cl)c(Cl)c2)CCC1N1CCCC(CNC(=O)c2ccc3ncccc3c2)C1 10.1016/j.bmcl.2005.04.054
44399332 69304 None 0 Human Functional pKi = 7.1 7.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 6 1 4 6.2 CC(c1ccc(Cl)c(Cl)c1)N1CCC(N2CCCC(CNC(=O)c3ccc4ncccc4c3)C2)CC1 10.1016/j.bmcl.2005.04.054
CHEMBL192757 69304 None 0 Human Functional pKi = 7.1 7.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 524 6 1 4 6.2 CC(c1ccc(Cl)c(Cl)c1)N1CCC(N2CCCC(CNC(=O)c3ccc4ncccc4c3)C2)CC1 10.1016/j.bmcl.2005.04.054
44399290 67633 None 0 Human Functional pKi = 6.1 6.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 538 6 1 4 5.2 O=C(NCC1CCCN(C2CCN(C(=O)Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL190312 67633 None 0 Human Functional pKi = 6.1 6.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 538 6 1 4 5.2 O=C(NCC1CCCN(C2CCN(C(=O)Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
44399567 67799 None 0 Human Functional pKi = 7.1 7.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccnc2ccccc12 10.1016/j.bmcl.2005.04.054
CHEMBL190852 67799 None 0 Human Functional pKi = 7.1 7.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 510 6 1 4 5.6 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1ccnc2ccccc12 10.1016/j.bmcl.2005.04.054
44399407 67589 None 0 Human Functional pKi = 7.1 7.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 487 7 1 3 5.3 Cc1ccccc1CC(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
CHEMBL189917 67589 None 0 Human Functional pKi = 7.1 7.1 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 487 7 1 3 5.3 Cc1ccccc1CC(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
44399442 67675 None 0 Human Functional pKi = 7.0 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 489 7 1 4 5.1 COc1ccccc1C(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
CHEMBL190646 67675 None 0 Human Functional pKi = 7.0 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 489 7 1 4 5.1 COc1ccccc1C(=O)NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2005.04.054
44399537 67640 None 0 Human Functional pKi = 7.0 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 476 6 1 4 5.0 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)cc3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
CHEMBL190362 67640 None 0 Human Functional pKi = 7.0 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 476 6 1 4 5.0 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)cc3)CC2)C1)c1ccc2ncccc2c1 10.1016/j.bmcl.2005.04.054
44399479 67603 None 0 Human Functional pKi = 7 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 511 6 1 5 5.0 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cnnc2ccccc12 10.1016/j.bmcl.2005.04.054
CHEMBL190048 67603 None 0 Human Functional pKi = 7 7.0 - 0
In vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligandIn vitro binding activity against C-C chemokine receptor type 3 using [35S]GTP-gamma-S, as radioligand
ChEMBL 511 6 1 5 5.0 O=C(NCC1CCCN(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C1)c1cnnc2ccccc12 10.1016/j.bmcl.2005.04.054
3536 3906 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Measuring antagonism of CCL11-induced chemotaxis <i>in vitro</i>.Measuring antagonism of CCL11-induced chemotaxis <i>in vitro</i>.
Guide to Pharmacology 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10854442
44560289 3906 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Measuring antagonism of CCL11-induced chemotaxis <i>in vitro</i>.Measuring antagonism of CCL11-induced chemotaxis <i>in vitro</i>.
Guide to Pharmacology 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10854442
CHEMBL1186993 3906 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Measuring antagonism of CCL11-induced chemotaxis <i>in vitro</i>.Measuring antagonism of CCL11-induced chemotaxis <i>in vitro</i>.
Guide to Pharmacology 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10854442
4382 833 None 0 Human Functional pIC50 = 7.5 7.5 25 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23951310
9680 1898 None 6 Human Functional pIC50 = 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 450 7 3 4 2.8 O=C(NCc1ccc(cc1)C(=O)N)NC[C@H]1OCCN(C1)Cc1ccc(c(c1)Cl)Cl 22931505
9825034 1898 None 6 Human Functional pIC50 = 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 450 7 3 4 2.8 O=C(NCc1ccc(cc1)C(=O)N)NC[C@H]1OCCN(C1)Cc1ccc(c(c1)Cl)Cl 22931505
CHEMBL2178574 1898 None 6 Human Functional pIC50 = 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 450 7 3 4 2.8 O=C(NCc1ccc(cc1)C(=O)N)NC[C@H]1OCCN(C1)Cc1ccc(c(c1)Cl)Cl 22931505
776 853 None 0 Human Functional pIC50 = 8.4 8.4 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488147
776 853 None 0 Human Functional pIC50 = 8.4 8.4 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
776 853 None 0 Human Functional pIC50 = 8.4 8.4 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16339911
754 830 None 0 Human Functional pIC50 = 8.6 8.6 5 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
775 849 None 0 Human Functional pIC50 = 8.7 8.7 316 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
775 849 None 0 Human Functional pIC50 = 8.7 8.7 316 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16339911
769 827 None 0 Human Functional pIC50 = 8.9 8.9 14 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488147
769 827 None 0 Human Functional pIC50 = 8.9 8.9 14 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10854442
769 827 None 0 Human Functional pIC50 = 8.9 8.9 14 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12761559
769 827 None 0 Human Functional pIC50 = 8.9 8.9 14 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16339911
769 827 None 0 Human Functional pIC50 = 8.9 8.9 14 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
770 828 None 0 Human Functional pIC50 = 9.5 9.5 7 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16339911
770 828 None 0 Human Functional pIC50 = 9.5 9.5 7 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
773 1937 None 0 Human Functional pIC50 None 7.2 7.2 -12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9789057
10098735 3343 None 0 Human Functional pIC50 None 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 537 10 2 5 6.1 COc1cc(NC(=O)N[C@H](C(C)C)CN2CCC(CC2)Cc2ccc(c(c2)Cl)Cl)cc(c1OC)OC 12070060
789 3343 None 0 Human Functional pIC50 None 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 537 10 2 5 6.1 COc1cc(NC(=O)N[C@H](C(C)C)CN2CCC(CC2)Cc2ccc(c(c2)Cl)Cl)cc(c1OC)OC 12070060
11556309 4120 None 0 Human Functional pIC50 None 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 502 5 2 5 3.9 O=C(C=C1CCN(CC1)C(=O)c1ncc(cc1O)C)N[C@@H]1CCN(C1)Cc1ccc2c(c1)ccc(c2)F 16339911
793 4120 None 0 Human Functional pIC50 None 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 502 5 2 5 3.9 O=C(C=C1CCN(CC1)C(=O)c1ncc(cc1O)C)N[C@@H]1CCN(C1)Cc1ccc2c(c1)ccc(c2)F 16339911
788 2494 None 0 Human Functional pIC50 None 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10640766
10304110 3349 None 0 Human Functional pIC50 None 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 560 11 2 7 5.3 COc1cc(ccc1OC)c1cnc(nc1)SCC(=O)NCC[C@H]1NC[C@@H](C1)Cc1ccc(c(c1)Cl)Cl 12070060
792 3349 None 0 Human Functional pIC50 None 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 560 11 2 7 5.3 COc1cc(ccc1OC)c1cnc(nc1)SCC(=O)NCC[C@H]1NC[C@@H](C1)Cc1ccc(c(c1)Cl)Cl 12070060
10255622 3347 None 0 Human Functional pIC50 None 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 505 10 3 6 4.2 COc1cc(NC(=O)N[C@H](C(O)C)CN2CCC(CC2)Cc2ccc(cc2)Cl)cc(c1OC)OC 12070060
791 3347 None 0 Human Functional pIC50 None 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 505 10 3 6 4.2 COc1cc(NC(=O)N[C@H](C(O)C)CN2CCC(CC2)Cc2ccc(cc2)Cl)cc(c1OC)OC 12070060
790 3344 None 0 Human Functional pIC50 None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 552 10 2 4 6.3 COc1cc(NC(=O)N[C@H](C(C)C)C[N+]2(C)CCC(CC2)Cc2ccc(c(c2)Cl)Cl)cc(c1OC)OC 12070060
9915610 3344 None 0 Human Functional pIC50 None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 552 10 2 4 6.3 COc1cc(NC(=O)N[C@H](C(C)C)C[N+]2(C)CCC(CC2)Cc2ccc(c(c2)Cl)Cl)cc(c1OC)OC 12070060


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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
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
38347547 146543 None 8 Human Binding pEC50 = 5.9 5.9 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 430 11 0 7 4.5 C=CCc1cc(OC)c(O[C@@H](C)[C@H](OC(C)=O)c2ccc(OC)c(OC)c2)c(OC)c1 10.1021/acs.jnatprod.6b00262
CHEMBL3922119 146543 None 8 Human Binding pEC50 = 5.9 5.9 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 430 11 0 7 4.5 C=CCc1cc(OC)c(O[C@@H](C)[C@H](OC(C)=O)c2ccc(OC)c(OC)c2)c(OC)c1 10.1021/acs.jnatprod.6b00262
25751147 150048 None 3 Human Binding pEC50 = 5.8 5.8 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 404 10 2 7 3.7 C=CCc1cc(OC)c(O[C@H](C)[C@@H](O)c2cc(OC)c(O)c(OC)c2)c(OC)c1 10.1021/acs.jnatprod.6b00262
CHEMBL3949874 150048 None 3 Human Binding pEC50 = 5.8 5.8 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 404 10 2 7 3.7 C=CCc1cc(OC)c(O[C@H](C)[C@@H](O)c2cc(OC)c(O)c(OC)c2)c(OC)c1 10.1021/acs.jnatprod.6b00262
124396489 144552 None 10 Human Binding pEC50 = 5.8 5.8 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 356 5 1 5 4.7 C/C=C/c1cc(OC)c2c(c1)[C@@H](C)[C@H](c1cc(OC)c(O)c(OC)c1)O2 10.1021/acs.jnatprod.6b00262
CHEMBL3906647 144552 None 10 Human Binding pEC50 = 5.8 5.8 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 356 5 1 5 4.7 C/C=C/c1cc(OC)c2c(c1)[C@@H](C)[C@H](c1cc(OC)c(O)c(OC)c1)O2 10.1021/acs.jnatprod.6b00262
10474776 113721 None 32 Human Binding pEC50 = 6.1 6.1 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1021/acs.jnatprod.6b00262
CHEMBL33227 113721 None 32 Human Binding pEC50 = 6.1 6.1 - 0
Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assayAntagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1021/acs.jnatprod.6b00262
11272103 124442 None 0 Rat Binding pIC50 = 11 11.0 - 0
Inhibition of eotaxin-induced chemotaxis of rat eosinophilsInhibition of eotaxin-induced chemotaxis of rat eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Rat Binding pIC50 = 11 11.0 - 0
Inhibition of eotaxin-induced chemotaxis of rat eosinophilsInhibition of eotaxin-induced chemotaxis of rat eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44570583 191051 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 550 7 2 8 3.3 CN1CC(C)(NC(=O)Nc2cccc(-c3nnnn3C)c2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL505914 191051 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 550 7 2 8 3.3 CN1CC(C)(NC(=O)Nc2cccc(-c3nnnn3C)c2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL518571 191051 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 550 7 2 8 3.3 CN1CC(C)(NC(=O)Nc2cccc(-c3nnnn3C)c2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
44570583 191051 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 550 7 2 8 3.3 CN1CC(C)(NC(=O)Nc2cccc(-c3nnnn3C)c2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL505914 191051 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 550 7 2 8 3.3 CN1CC(C)(NC(=O)Nc2cccc(-c3nnnn3C)c2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL518571 191051 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 550 7 2 8 3.3 CN1CC(C)(NC(=O)Nc2cccc(-c3nnnn3C)c2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
44593547 176971 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 538 10 2 8 3.3 CCN(CCCc1ccc(F)cc1)CC1OC(=O)N(C)CC1(C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2008.11.002
CHEMBL461445 176971 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 538 10 2 8 3.3 CCN(CCCc1ccc(F)cc1)CC1OC(=O)N(C)CC1(C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2008.11.002
44447136 94605 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 469 11 3 7 2.8 CCN(CCCc1ccc(F)cc1)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL251837 94605 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 469 11 3 7 2.8 CCN(CCCc1ccc(F)cc1)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447381 94944 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 511 12 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)[C@@H](C)CCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254095 94944 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 511 12 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)[C@@H](C)CCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447137 154242 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 483 12 3 7 3.2 CCCN(CCCc1ccc(F)cc1)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL398548 154242 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 483 12 3 7 3.2 CCCN(CCCc1ccc(F)cc1)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44570537 178264 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 536 7 2 8 2.9 CN1C[C@@H](NC(=O)Nc2cccc(-c3nnnn3C)c2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL464902 178264 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 536 7 2 8 2.9 CN1C[C@@H](NC(=O)Nc2cccc(-c3nnnn3C)c2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
10050884 154742 None 15 Human Binding pIC50 = 9.5 9.5 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.11.002
CHEMBL399495 154742 None 15 Human Binding pIC50 = 9.5 9.5 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.11.002
44447143 94641 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 469 11 4 7 2.7 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CNCCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL252035 94641 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 469 11 4 7 2.7 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CNCCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
10050884 154742 None 15 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.087
CHEMBL399495 154742 None 15 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.087
44447144 168875 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 483 11 3 7 3.0 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(C)CCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL437396 168875 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 483 11 3 7 3.0 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(C)CCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
10050884 154742 None 15 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL399495 154742 None 15 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
44455658 167369 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 8 3 5 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nccn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL429323 167369 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 8 3 5 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nccn2C)c1 10.1016/j.bmcl.2007.11.067
11488078 79032 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113077 79032 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44593553 178472 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 489 6 2 6 3.9 Cc1csc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1016/j.bmcl.2008.11.002
CHEMBL465272 178472 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 489 6 2 6 3.9 Cc1csc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1016/j.bmcl.2008.11.002
44447139 94606 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 495 12 3 7 3.2 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)CC1CC1 10.1016/j.bmcl.2007.11.087
CHEMBL251838 94606 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 495 12 3 7 3.2 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)CC1CC1 10.1016/j.bmcl.2007.11.087
44447135 94729 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 455 10 3 7 2.5 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(C)CCCc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
CHEMBL252631 94729 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 455 10 3 7 2.5 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(C)CCCc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
44447361 95006 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H]([C@@H](O)c1ccccc1)N(C)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254503 95006 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H]([C@@H](O)c1ccccc1)N(C)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447138 154907 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 481 11 3 7 3.0 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)C1CC1 10.1016/j.bmcl.2007.11.087
CHEMBL400378 154907 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 481 11 3 7 3.0 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)C1CC1 10.1016/j.bmcl.2007.11.087
44447382 166708 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 497 12 3 7 3.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)CCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL428062 166708 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 497 12 3 7 3.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)CCCc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
10050884 154742 None 15 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3/CCR2 chimeric receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3/CCR2 chimeric receptor in CHO cells
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.087
CHEMBL399495 154742 None 15 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I] eotaxin from human CCR3/CCR2 chimeric receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3/CCR2 chimeric receptor in CHO cells
ChEMBL 481 8 3 7 2.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.087
44455841 155535 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 509 9 3 7 3.8 CC(C)[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL403838 155535 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 509 9 3 7 3.8 CC(C)[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11328714 79029 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113074 79029 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44593547 176971 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 538 10 2 8 3.3 CCN(CCCc1ccc(F)cc1)CC1OC(=O)N(C)CC1(C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2008.11.002
CHEMBL461445 176971 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 538 10 2 8 3.3 CCN(CCCc1ccc(F)cc1)CC1OC(=O)N(C)CC1(C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2008.11.002
44419331 82806 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 453 9 3 4 4.7 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL217987 82806 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 453 9 3 4 4.7 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
25032958 94601 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 481 10 4 8 2.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(C)[C@@H](C)[C@@H](O)c2ccccc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL251822 94601 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 481 10 4 8 2.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(C)[C@@H](C)[C@@H](O)c2ccccc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447145 95030 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 511 13 3 7 3.8 CCCN(CCCc1ccc(F)cc1)C[C@H](O)[C@@H](C)NC(=O)Nc1cc(CC)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254676 95030 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 511 13 3 7 3.8 CCCN(CCCc1ccc(F)cc1)C[C@H](O)[C@@H](C)NC(=O)Nc1cc(CC)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44455744 95484 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 495 8 3 7 3.5 Cc1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257029 95484 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 495 8 3 7 3.5 Cc1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455817 155268 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 538 9 3 8 3.6 CNC(=O)O[C@H](C[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)N1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL402331 155268 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 538 9 3 8 3.6 CNC(=O)O[C@H](C[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)N1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
44455788 155708 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 536 10 2 7 4.3 CCc1cc(NC(=O)N[C@H](C)C[C@@H](N(C)C)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL404585 155708 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 536 10 2 7 4.3 CCc1cc(NC(=O)N[C@H](C)C[C@@H](N(C)C)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11329244 71140 None 6 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of [125I]eotaxin binding to human eosinophilsInhibition of [125I]eotaxin binding to human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71140 None 6 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of [125I]eotaxin binding to human eosinophilsInhibition of [125I]eotaxin binding to human eosinophils
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11272103 124442 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of [125I]eotaxin binding to human eosinophilsInhibition of [125I]eotaxin binding to human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of [125I]eotaxin binding to human eosinophilsInhibition of [125I]eotaxin binding to human eosinophils
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
6918497 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(03)00748-0
CHEMBL277930 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(03)00748-0
CHEMBL331897 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(03)00748-0
6918497 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL277930 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL331897 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(01)00176-7
6918497 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory activity against I-Eotaxin binding to human CCR3 receptorsInhibitory activity against I-Eotaxin binding to human CCR3 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory activity against I-Eotaxin binding to human CCR3 receptorsInhibitory activity against I-Eotaxin binding to human CCR3 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory activity against I-Eotaxin binding to human CCR3 receptorsInhibitory activity against I-Eotaxin binding to human CCR3 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
11236950 94817 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 479 9 2 6 4.3 CN(CCCc1ccc(F)cc1)C[C@@H]1CCCC[C@H]1NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL253210 94817 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 479 9 2 6 4.3 CN(CCCc1ccc(F)cc1)C[C@@H]1CCCC[C@H]1NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447146 95031 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 509 12 3 7 3.5 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)C2CC2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254677 95031 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 509 12 3 7 3.5 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)C2CC2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447147 95058 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 523 13 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC2CC2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254881 95058 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 523 13 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC2CC2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44445886 94272 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 544 7 3 6 3.9 CNC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL249857 94272 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 544 7 3 6 3.9 CNC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
44455844 97469 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 509 10 3 7 4.0 CCC[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL269933 97469 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 509 10 3 7 4.0 CCC[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455791 155709 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 522 9 3 7 3.3 CC(=O)N[C@H](C[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)N1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
CHEMBL404586 155709 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 522 9 3 7 3.3 CC(=O)N[C@H](C[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)N1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2007.11.067
44289927 168430 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL43423 168430 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
11698698 123307 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 481 8 2 6 4.2 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3cccc(Cl)c3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL361369 123307 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 481 8 2 6 4.2 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3cccc(Cl)c3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44289927 168430 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43423 168430 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44390955 123757 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 493 8 2 6 4.3 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CCC2(C)C)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL362179 123757 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 493 8 2 6 4.3 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CCC2(C)C)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44419344 141860 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 495 11 2 4 5.9 CCCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL386073 141860 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 495 11 2 4 5.9 CCCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
11272103 124442 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL363840 124442 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
44445865 154944 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 544 7 3 6 3.9 CNC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL400589 154944 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 544 7 3 6 3.9 CNC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
44455461 155712 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 551 10 3 7 4.2 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)C(=O)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL404618 155712 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 551 10 3 7 4.2 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)C(=O)O)c1 10.1016/j.bmcl.2007.11.067
44390838 128577 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL366710 128577 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11398022 98684 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
CHEMBL277131 98684 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
11272103 124442 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11397114 133537 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2cn[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL3706810 133537 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2cn[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
10459751 100227 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 533 9 2 10 2.7 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
CHEMBL288009 100227 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 533 9 2 10 2.7 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
44289701 101160 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 508 9 3 7 2.8 CNC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
CHEMBL295081 101160 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 508 9 3 7 2.8 CNC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
44455793 95280 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 483 9 3 5 4.4 CC(=O)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL256068 95280 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 483 9 3 5 4.4 CC(=O)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
44455625 97643 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 565 9 3 7 6.2 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nccs2)cc(-c2nccs2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270806 97643 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 565 9 3 7 6.2 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nccs2)cc(-c2nccs2)c1 10.1016/j.bmcl.2007.11.067
11227406 94398 None 2 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]eotaxin binding to human eosinophilsInhibition of [125I]eotaxin binding to human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL250689 94398 None 2 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]eotaxin binding to human eosinophilsInhibition of [125I]eotaxin binding to human eosinophils
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44419295 83247 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 497 11 3 5 4.4 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCO)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218568 83247 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 497 11 3 5 4.4 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCO)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44419298 138226 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 509 11 2 5 5.0 CC(=O)CN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL376737 138226 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 509 11 2 5 5.0 CC(=O)CN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
11329244 71140 None 6 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL195433 71140 None 6 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445863 94508 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 559 9 2 7 3.7 COCC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL251275 94508 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 559 9 2 7 3.7 COCC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
44445872 94566 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 533 9 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CCF)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251622 94566 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 533 9 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CCF)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445868 167071 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 567 9 2 7 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(Cc3ccco3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL428761 167071 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 567 9 2 7 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(Cc3ccco3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11329244 71140 None 6 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71140 None 6 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11156406 125238 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL364508 125238 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44290100 178726 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 481 9 3 7 3.0 Cn1nnnc1-c1cc(CO)cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL46747 178726 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 481 9 3 7 3.0 Cn1nnnc1-c1cc(CO)cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44419345 83186 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 493 11 2 4 5.6 C=CCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218262 83186 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 493 11 2 4 5.6 C=CCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
11272103 124442 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.087
CHEMBL363840 124442 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.087
44445842 155667 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 488 7 2 6 4.3 CC(=O)c1sc(NC(=O)N[C@@H]2COCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL404416 155667 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 488 7 2 6 4.3 CC(=O)c1sc(NC(=O)N[C@@H]2COCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455686 95545 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 523 9 3 7 4.3 CC(C)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257293 95545 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 523 9 3 7 4.3 CC(C)c1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455871 97599 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 495 9 3 7 3.6 CC[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270583 97599 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 495 9 3 7 3.6 CC[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11272103 124442 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL363840 124442 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
44455511 155117 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 9 2 6 4.0 CCc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL401545 155117 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 9 2 6 4.0 CCc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44295462 188516 None 0 Human Binding pIC50 = 9 9.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 519 12 3 7 4.3 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50194 188516 None 0 Human Binding pIC50 = 9 9.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 519 12 3 7 4.3 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/s0960-894x(02)00206-8
44295536 188542 None 0 Human Binding pIC50 = 9 9.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 12 3 4 5.3 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50233 188542 None 0 Human Binding pIC50 = 9 9.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 12 3 4 5.3 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
9892753 16507 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 516 8 3 4 5.5 CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm049530m
CHEMBL123611 16507 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 516 8 3 4 5.5 CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm049530m
11213416 133539 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2nc[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL3706812 133539 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2nc[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11169258 140984 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 587 8 2 10 3.8 Cn1nnnc1-c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1021/jm049530m
CHEMBL382108 140984 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 587 8 2 10 3.8 Cn1nnnc1-c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1021/jm049530m
11966688 12376 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 518 7 2 4 6.0 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2C[N+]2(C)CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL1185532 12376 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 518 7 2 4 6.0 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2C[N+]2(C)CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL419599 12376 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 518 7 2 4 6.0 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2C[N+]2(C)CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
9892753 16507 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 516 8 3 4 5.5 CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL123611 16507 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 516 8 3 4 5.5 CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
11730796 116892 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 499 7 3 4 5.2 CNC(=O)c1cccc(NC(=O)Nc2cccc(C#N)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL337962 116892 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 499 7 3 4 5.2 CNC(=O)c1cccc(NC(=O)Nc2cccc(C#N)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44570617 178481 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 531 7 2 7 4.1 CC(=O)c1sc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2008.11.002
CHEMBL465291 178481 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 531 7 2 7 4.1 CC(=O)c1sc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2008.11.002
44445885 169111 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 558 8 3 6 4.3 CCNC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL439253 169111 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 558 8 3 6 4.3 CCNC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
44455483 97882 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 537 10 3 7 3.8 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)(C)C(=O)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL272068 97882 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 537 10 3 7 3.8 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)(C)C(=O)O)c1 10.1016/j.bmcl.2007.11.067
44455458 167555 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 533 9 3 7 5.3 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2ccon2)cc(-c2ccon2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL429846 167555 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 533 9 3 7 5.3 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2ccon2)cc(-c2ccon2)c1 10.1016/j.bmcl.2007.11.067
44400941 68886 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 426 6 3 3 3.9 O=C(NC1C=CC=CN1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL192240 68886 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 426 6 3 3 3.9 O=C(NC1C=CC=CN1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11409583 69804 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 507 8 2 4 5.9 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1021/jm049530m
CHEMBL193575 69804 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 507 8 2 4 5.9 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1021/jm049530m
44445901 160301 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 501 7 2 6 4.2 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2008.11.002
CHEMBL410959 160301 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 501 7 2 6 4.2 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2008.11.002
44447375 94823 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 527 12 4 8 2.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)[C@@H](C)[C@@H](O)Cc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL253244 94823 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 527 12 4 8 2.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)[C@@H](C)[C@@H](O)Cc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44445854 94136 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 522 7 2 7 3.3 CC(=O)c1sc(NC(=O)N[C@@H]2CS(=O)(=O)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249057 94136 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 522 7 2 7 3.3 CC(=O)c1sc(NC(=O)N[C@@H]2CS(=O)(=O)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445891 94473 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 533 9 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CCF)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251044 94473 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 533 9 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CCF)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445915 155519 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 599 8 2 7 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C3CCOCC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL403742 155519 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 599 8 2 7 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C3CCOCC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445888 155749 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 526 8 2 7 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CC#N)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL404857 155749 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 526 8 2 7 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CC#N)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445901 160301 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 501 7 2 6 4.2 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL410959 160301 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 501 7 2 6 4.2 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455818 95494 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 523 10 3 7 4.2 CC(C)C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257073 95494 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 523 10 3 7 4.2 CC(C)C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455510 95643 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 8 2 6 4.2 Cc1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257737 95643 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 8 2 6 4.2 Cc1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455790 95775 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 480 8 3 7 3.2 C[C@H](C[C@@H](N)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL258322 95775 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 480 8 3 7 3.2 C[C@H](C[C@@H](N)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44289926 177664 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 453 9 2 4 4.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL46404 177664 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 453 9 2 4 4.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
44390883 64095 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.8 CCc1cc(NC(=O)N[C@@H]2CCCN(CCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180746 64095 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.8 CCc1cc(NC(=O)N[C@@H]2CCCN(CCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11167549 79031 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 480 6 2 4 6.1 O=C(Nc1ccc2ncsc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113076 79031 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 480 6 2 4 6.1 O=C(Nc1ccc2ncsc2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44290018 166800 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 465 9 2 6 4.0 CCn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42826 166800 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 465 9 2 6 4.0 CCn1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44289741 170833 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 519 8 2 6 4.5 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.059
CHEMBL44522 170833 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 519 8 2 6 4.5 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.059
44289926 177664 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 453 9 2 4 4.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2004.01.059
CHEMBL46404 177664 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 453 9 2 4 4.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2004.01.059
44419296 141537 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 511 12 3 5 4.8 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCCO)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL384199 141537 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 511 12 3 5 4.8 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCCO)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44445884 94270 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 559 9 2 7 3.7 COCC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL249855 94270 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 559 9 2 7 3.7 COCC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
44445867 94345 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 526 8 2 7 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CC#N)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL250437 94345 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 526 8 2 7 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CC#N)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
16747712 154943 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(C)=O)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL400588 154943 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(C)=O)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445870 167360 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 9 2 7 4.1 CC(=O)CN1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL429303 167360 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 9 2 7 4.1 CC(=O)CN1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
44455539 167078 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 8 2 6 3.9 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL428775 167078 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 8 2 6 3.9 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
10096657 64875 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 8 2 6 3.9 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2C)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL182086 64875 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 8 2 6 3.9 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2C)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11306550 79034 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 497 6 3 3 6.0 O=C(Nc1ccc2[nH]nc(Cl)c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113079 79034 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 497 6 3 3 6.0 O=C(Nc1ccc2[nH]nc(Cl)c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44419328 83340 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 411 8 3 3 4.5 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL219048 83340 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 411 8 3 3 4.5 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
44445895 94502 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 584 8 2 7 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C3CCN(C)CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251220 94502 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 584 8 2 7 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C3CCN(C)CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455482 97881 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 533 9 3 9 3.2 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2ccnn2)cc(-n2ccnn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL272067 97881 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 533 9 3 9 3.2 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2ccnn2)cc(-n2ccnn2)c1 10.1016/j.bmcl.2007.11.067
11363005 60526 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL175634 60526 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11442162 70692 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 444 6 2 4 5.2 Cc1csc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1021/jm049530m
CHEMBL195044 70692 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 444 6 2 4 5.2 Cc1csc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1021/jm049530m
11454941 71166 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cc1nnnn1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL195555 71166 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 505 7 2 6 4.7 Cc1nnnn1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44445864 94535 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 558 8 3 6 4.3 CCNC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL251446 94535 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 558 8 3 6 4.3 CCNC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
44445916 155520 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 599 8 2 7 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C3CCOCC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL403743 155520 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 599 8 2 7 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C3CCOCC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455820 95495 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 551 11 3 7 4.9 CCC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL257074 95495 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 551 11 3 7 4.9 CCC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
44455869 97598 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 507 9 2 7 4.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270582 97598 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 507 9 2 7 4.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44289715 170338 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 8 2 6 3.8 Cc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL444568 170338 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 8 2 6 3.8 Cc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11340670 127301 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 483 7 2 3 5.8 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)ccc1F 10.1021/jm049530m
CHEMBL365820 127301 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 483 7 2 3 5.8 CC(=O)c1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)ccc1F 10.1021/jm049530m
44289715 170338 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 465 8 2 6 3.8 Cc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
CHEMBL444568 170338 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 465 8 2 6 3.8 Cc1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
44445887 94273 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)CN(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249858 94273 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)CN(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445866 155053 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)CN(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL401159 155053 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)CN(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455847 155536 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 501 9 2 6 4.7 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL403839 155536 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 501 9 2 6 4.7 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
10322255 62547 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL178230 62547 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44390945 62969 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 507 9 2 6 4.5 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2C(C)C)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL178503 62969 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 507 9 2 6 4.5 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2C(C)C)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11154845 60737 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 6 2 2 5.8 Cc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL176077 60737 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 6 2 2 5.8 Cc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11454015 133540 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2cc[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL3706813 133540 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2cc[nH]c2c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
16126667 83098 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 425 8 2 3 4.9 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2C)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218174 83098 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 425 8 2 3 4.9 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2C)c1 10.1016/j.bmcl.2006.08.012
44445839 155610 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 488 7 2 6 4.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCO[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL404213 155610 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 488 7 2 6 4.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCO[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455846 97513 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 515 9 2 6 5.1 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270147 97513 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 515 9 2 6 5.1 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
44455765 155450 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 543 8 2 6 4.6 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(Br)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL403331 155450 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 543 8 2 6 4.6 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(Br)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11751629 79035 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 464 6 3 3 5.4 O=C(Nc1ccc2c(c1)CCN2)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113080 79035 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 464 6 3 3 5.4 O=C(Nc1ccc2c(c1)CCN2)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
10458976 95064 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 509 9 3 7 3.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254930 95064 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 509 9 3 7 3.4 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44445873 155054 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CC(=O)N(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL401160 155054 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CC(=O)N(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455766 95738 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 8 2 6 4.3 C[C@H](C[C@@H](C)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL258156 95738 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 8 2 6 4.3 C[C@H](C[C@@H](C)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455745 155391 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 559 8 3 7 4.0 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(Br)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL402983 155391 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 559 8 3 7 4.0 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(Br)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455711 168836 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 509 9 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL437031 168836 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 509 9 3 7 3.8 CCc1cc(NC(=O)N[C@H](C)C[C@@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44390938 62975 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 483 8 2 6 3.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3F)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL178506 62975 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 483 8 2 6 3.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3F)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11351206 69445 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 441 6 2 2 5.6 O=C(Nc1ccccc1F)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL193330 69445 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 441 6 2 2 5.6 O=C(Nc1ccccc1F)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11477384 133538 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 490 6 3 2 6.6 Cc1[nH]c2cc(NC(=O)N[C@@H]3CCCC[C@H]3CN3CCC[C@@H](Cc4ccc(F)cc4)C3)ccc2c1C 10.1021/jm049530m
CHEMBL3706811 133538 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 490 6 3 2 6.6 Cc1[nH]c2cc(NC(=O)N[C@@H]3CCCC[C@H]3CN3CCC[C@@H](Cc4ccc(F)cc4)C3)ccc2c1C 10.1021/jm049530m
44419301 84116 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 491 10 2 4 5.1 C#CCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220765 84116 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 491 10 2 4 5.1 C#CCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
11953409 94269 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249854 94269 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445845 94295 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CCNC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL250056 94295 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CCNC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390837 63569 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 9 2 6 4.0 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180042 63569 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 9 2 6 4.0 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11419003 70932 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 430 6 2 4 4.9 O=C(Nc1nccs1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL195129 70932 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 430 6 2 4 4.9 O=C(Nc1nccs1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44401328 71120 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL195348 71120 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 462 6 3 2 5.9 O=C(Nc1ccc2[nH]ccc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
11373714 127242 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 427 6 2 4 4.2 Cn1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1021/jm049530m
CHEMBL365732 127242 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 427 6 2 4 4.2 Cn1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1021/jm049530m
9680 1898 None 6 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 450 7 3 4 2.8 O=C(NCc1ccc(cc1)C(=O)N)NC[C@H]1OCCN(C1)Cc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
9825034 1898 None 6 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 450 7 3 4 2.8 O=C(NCc1ccc(cc1)C(=O)N)NC[C@H]1OCCN(C1)Cc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
CHEMBL2178574 1898 None 6 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 450 7 3 4 2.8 O=C(NCc1ccc(cc1)C(=O)N)NC[C@H]1OCCN(C1)Cc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
22393282 101260 None 0 Human Binding pIC50 = 8 8.0 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL295832 101260 None 0 Human Binding pIC50 = 8 8.0 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
22393282 101260 None 0 Human Binding pIC50 = 8 8.0 - 1
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL295832 101260 None 0 Human Binding pIC50 = 8 8.0 - 1
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
11385178 124874 None 0 Human Binding pIC50 = 8 8.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 441 6 2 2 5.6 O=C(Nc1cccc(F)c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL364263 124874 None 0 Human Binding pIC50 = 8 8.0 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 441 6 2 2 5.6 O=C(Nc1cccc(F)c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
22393282 101260 None 0 Human Binding pIC50 = 8 8.0 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL295832 101260 None 0 Human Binding pIC50 = 8 8.0 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
44440398 93386 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 584 8 0 5 6.3 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(C2CCCCC2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL245310 93386 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 584 8 0 5 6.3 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(C2CCCCC2)n1C 10.1016/j.bmcl.2007.05.035
44440420 93585 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 608 9 0 6 5.8 COc1ccc(-n2c(=O)c(CN(CCc3ccc(Cl)cc3)C3CCN(C(=O)c4c(F)cccc4F)CC3)c(C)n2C)cc1 10.1016/j.bmcl.2007.05.035
CHEMBL246347 93585 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 608 9 0 6 5.8 COc1ccc(-n2c(=O)c(CN(CCc3ccc(Cl)cc3)C3CCN(C(=O)c4c(F)cccc4F)CC3)c(C)n2C)cc1 10.1016/j.bmcl.2007.05.035
44440424 149348 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 621 9 0 6 5.8 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(N(C)C)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL394443 149348 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 621 9 0 6 5.8 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(N(C)C)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440426 149351 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 613 8 0 6 5.8 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2cnccc2Cl)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL394444 149351 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 613 8 0 6 5.8 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2cnccc2Cl)n1C 10.1016/j.bmcl.2007.05.035
44440411 150178 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2cccc(F)c2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL395090 150178 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2cccc(F)c2)n1C 10.1016/j.bmcl.2007.05.035
44440414 151112 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 594 8 1 6 5.5 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(O)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL395851 151112 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 594 8 1 6 5.5 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(O)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440417 151115 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 623 9 0 7 5.7 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc([N+](=O)[O-])cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL395852 151115 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 623 9 0 7 5.7 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc([N+](=O)[O-])cc2)n1C 10.1016/j.bmcl.2007.05.035
44295264 187581 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 8 2 3 5.6 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(-c2ccco2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL49404 187581 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 8 2 3 5.6 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(-c2ccco2)c1 10.1016/s0960-894x(02)00206-8
44295664 188802 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 10 2 3 5.5 CCC[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50423 188802 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 10 2 3 5.5 CCC[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
44295405 189190 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 8 3 3 4.7 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(-c2ncc[nH]2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50988 189190 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 8 3 3 4.7 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(-c2ncc[nH]2)c1 10.1016/s0960-894x(02)00206-8
22393436 189419 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 375 7 2 2 4.1 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NC1CCCCC1 10.1016/s0960-894x(02)00206-8
CHEMBL51229 189419 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 375 7 2 2 4.1 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NC1CCCCC1 10.1016/s0960-894x(02)00206-8
44295567 190762 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 465 10 3 4 4.7 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@H](O)C(C)C)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51815 190762 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 465 10 3 4 4.7 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@H](O)C(C)C)c1 10.1016/s0960-894x(02)00206-8
9979012 79833 None 0 Human Binding pIC50 = 6 6.0 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 411 7 1 5 4.4 O=C(CSc1nc2ccccc2s1)NCC1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(01)00176-7
CHEMBL21199 79833 None 0 Human Binding pIC50 = 6 6.0 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 411 7 1 5 4.4 O=C(CSc1nc2ccccc2s1)NCC1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(01)00176-7
44273640 98982 None 0 Human Binding pIC50 = 6 6.0 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 417 7 1 5 4.8 O=C(CSc1nc2ccccc2s1)NCC1CCCN(CC2CCCCC2)C1 10.1016/s0960-894x(01)00176-7
CHEMBL279450 98982 None 0 Human Binding pIC50 = 6 6.0 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 417 7 1 5 4.8 O=C(CSc1nc2ccccc2s1)NCC1CCCN(CC2CCCCC2)C1 10.1016/s0960-894x(01)00176-7
57401421 67887 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
CHEMBL1910161 67887 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
44440435 93492 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 563 8 0 6 4.6 Cc1c(CN(CCc2ccccn2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL245956 93492 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 563 8 0 6 4.6 Cc1c(CN(CCc2ccccn2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44295529 187406 None 0 Human Binding pIC50 = 6 6.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 368 8 1 2 4.3 O=C(NCCCCN1CCC(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL49296 187406 None 0 Human Binding pIC50 = 6 6.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 368 8 1 2 4.3 O=C(NCCCCN1CCC(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
44349617 118182 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 336 4 0 2 4.0 Fc1ccc(CCCN2CCC3C(C2)c2cccc4c2N3CC4)cc1 10.1021/jm0201767
CHEMBL340770 118182 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 336 4 0 2 4.0 Fc1ccc(CCCN2CCC3C(C2)c2cccc4c2N3CC4)cc1 10.1021/jm0201767
5481702 208281 None 0 Human Binding pIC50 = 5 5.0 - 0
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR3 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR3 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 208281 None 0 Human Binding pIC50 = 5 5.0 - 0
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR3 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR3 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
44442590 93825 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93825 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44295435 189762 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 415 6 1 4 2.7 O=S(=O)(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51512 189762 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 415 6 1 4 2.7 O=S(=O)(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
44346194 15555 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 501 9 2 5 5.4 COc1cc(NC(=O)N[C@H](C)CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
CHEMBL121905 15555 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 501 9 2 5 5.4 COc1cc(NC(=O)N[C@H](C)CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
11006582 11460 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 483 6 2 4 5.5 C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL1180359 11460 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 483 6 2 4 5.5 C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL123616 11460 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 483 6 2 4 5.5 C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccccc2)CC1 10.1021/jm0201767
11059789 16779 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 472 7 3 4 5.3 N#Cc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL124438 16779 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 472 7 3 4 5.3 N#Cc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
10983981 16855 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 505 8 2 5 5.7 COC(=O)c1cccc(NC(=O)Nc2cccc(OC)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL124821 16855 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 505 8 2 5 5.7 COC(=O)c1cccc(NC(=O)Nc2cccc(OC)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
10895831 118477 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 461 8 2 3 6.0 COc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL341074 118477 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 461 8 2 3 6.0 COc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44295486 101554 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 502 5 2 3 4.0 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)Nc1cccc(I)c1 10.1016/s0960-894x(02)00206-8
CHEMBL297945 101554 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 502 5 2 3 4.0 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)Nc1cccc(I)c1 10.1016/s0960-894x(02)00206-8
20576924 189348 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 364 5 0 3 4.0 O=C(CCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51163 189348 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 364 5 0 3 4.0 O=C(CCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
45270199 198874 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Inhibition of mouse CCR3Inhibition of mouse CCR3
ChEMBL 516 5 1 4 4.2 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1cc[n+]([O-])cc1C(=O)N1CCCCC1 10.1016/j.bmc.2009.06.066
CHEMBL562897 198874 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Inhibition of mouse CCR3Inhibition of mouse CCR3
ChEMBL 516 5 1 4 4.2 O=C(NC1CC2CCC(C1)N2Cc1ccc2cc(F)ccc2c1)c1cc[n+]([O-])cc1C(=O)N1CCCCC1 10.1016/j.bmc.2009.06.066
44295408 188907 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 381 6 1 3 3.7 O=C(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)C1CCCCC1 10.1016/s0960-894x(02)00206-8
CHEMBL50591 188907 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 381 6 1 3 3.7 O=C(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)C1CCCCC1 10.1016/s0960-894x(02)00206-8
11101888 113369 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 421 5 2 2 6.0 O=C(Nc1cc(F)ccc1F)Nc1ccccc1CN1CCC(c2ccccc2)CC1 10.1021/jm0201767
CHEMBL331530 113369 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 421 5 2 2 6.0 O=C(Nc1cc(F)ccc1F)Nc1ccccc1CN1CCC(c2ccccc2)CC1 10.1021/jm0201767
10983308 17984 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 454 7 3 4 5.1 N#Cc1cccc(NC(=O)Nc2cc(CO)ccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL126174 17984 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 454 7 3 4 5.1 N#Cc1cccc(NC(=O)Nc2cc(CO)ccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
57392726 67893 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 490 8 0 5 4.2 COc1ccc(OC)c(S(=O)(=O)N2CCC(CN3CCC(Cc4ccc(F)cc4)CC3)CC2)c1 10.1016/j.bmcl.2011.09.013
CHEMBL1910167 67893 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 490 8 0 5 4.2 COc1ccc(OC)c(S(=O)(=O)N2CCC(CN3CCC(Cc4ccc(F)cc4)CC3)CC2)c1 10.1016/j.bmcl.2011.09.013
44346153 15510 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 519 8 3 5 4.1 C[C@H](O)[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
CHEMBL121637 15510 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 519 8 3 5 4.1 C[C@H](O)[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
44346154 168764 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 489 7 2 4 4.7 C[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
CHEMBL436363 168764 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 489 7 2 4 4.7 C[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
44440437 146551 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 600 9 0 8 4.9 Cc1ccnc(C)c1C(=O)N1CCC(N(CCc2ccc([N+](=O)[O-])cc2)Cc2c(C)n(C)n(-c3ccc(F)cc3)c2=O)CC1 10.1016/j.bmcl.2007.05.035
CHEMBL392218 146551 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 600 9 0 8 4.9 Cc1ccnc(C)c1C(=O)N1CCC(N(CCc2ccc([N+](=O)[O-])cc2)Cc2c(C)n(C)n(-c3ccc(F)cc3)c2=O)CC1 10.1016/j.bmcl.2007.05.035
23657036 146552 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 572 9 0 8 4.3 Cc1c(CN(CCc2ccc([N+](=O)[O-])cc2)C2CCN(C(=O)c3ccccn3)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL392219 146552 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 572 9 0 8 4.3 Cc1c(CN(CCc2ccc([N+](=O)[O-])cc2)C2CCN(C(=O)c3ccccn3)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44390848 122456 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3cccc(F)c3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL360062 122456 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3cccc(F)c3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
9868532 60507 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL175502 60507 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
11396995 70326 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 459 6 2 2 5.7 O=C(Nc1ccc(F)c(F)c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL194384 70326 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 459 6 2 2 5.7 O=C(Nc1ccc(F)c(F)c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44387837 123899 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 448 6 2 3 5.3 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL362465 123899 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 448 6 2 3 5.3 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
44419303 141934 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 517 11 2 4 5.7 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC(F)F)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL386493 141934 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 517 11 2 4 5.7 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC(F)F)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44390843 64200 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 477 9 2 7 3.5 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(OC)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180860 64200 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 477 9 2 7 3.5 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(OC)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44295374 101646 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 404 9 2 3 4.8 N#Cc1cccc(NC(=O)NCCCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL298681 101646 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 404 9 2 3 4.8 N#Cc1cccc(NC(=O)NCCCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44295352 188791 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 380 9 1 3 4.2 COc1cccc(C(=O)NCCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50400 188791 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 380 9 1 3 4.2 COc1cccc(C(=O)NCCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44295372 189272 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 419 7 2 2 5.2 O=C(NCCCN1CCC(Cc2ccccc2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51113 189272 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 419 7 2 2 5.2 O=C(NCCCN1CCC(Cc2ccccc2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(02)00206-8
10623381 16909 None 0 Human Binding pIC50 = 4.9 4.9 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 448 8 2 3 5.3 NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL125111 16909 None 0 Human Binding pIC50 = 4.9 4.9 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 448 8 2 3 5.3 NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44349204 17215 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 350 5 0 2 3.8 CC1C2=C(CC=CC2)C(=O)N1CC1CCN(CCc2ccccc2)CC1 10.1021/jm0201767
CHEMBL125643 17215 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 350 5 0 2 3.8 CC1C2=C(CC=CC2)C(=O)N1CC1CCN(CCc2ccccc2)CC1 10.1021/jm0201767
11037869 16730 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 459 7 2 3 6.1 CC(=O)c1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL124317 16730 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 459 7 2 3 6.1 CC(=O)c1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
11037869 16730 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 459 7 2 3 6.1 CC(=O)c1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL124317 16730 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 459 7 2 3 6.1 CC(=O)c1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44419314 83333 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218997 83333 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
44593553 178472 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 489 6 2 6 3.9 Cc1csc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1016/j.bmcl.2008.11.002
CHEMBL465272 178472 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 489 6 2 6 3.9 Cc1csc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1016/j.bmcl.2008.11.002
44390891 63995 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NC[C@H]2CCCN(CCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180694 63995 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NC[C@H]2CCCN(CCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
44295544 189038 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 375 8 1 3 4.0 N#Cc1ccc(C(=O)NCCCCN2CCC(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL50801 189038 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 375 8 1 3 4.0 N#Cc1ccc(C(=O)NCCCCN2CCC(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
11826382 17279 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 443 8 2 3 5.5 COc1ccc(NC(=O)NCc2ccccc2CN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
CHEMBL125695 17279 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 443 8 2 3 5.5 COc1ccc(NC(=O)NCc2ccccc2CN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
44419305 82663 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 535 10 2 4 6.0 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC(F)(F)F)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL217928 82663 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 535 10 2 4 6.0 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC(F)(F)F)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44390867 62599 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 7 2 6 3.4 CCc1cc(NC(=O)N[C@@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL178278 62599 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 7 2 6 3.4 CCc1cc(NC(=O)N[C@@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11396851 60517 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL175559 60517 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
11247999 77999 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL2096763 77999 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
10972522 17137 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 456 7 2 3 5.8 N#Cc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL125549 17137 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 456 7 2 3 5.8 N#Cc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
11004663 117666 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 438 7 2 3 5.7 N#Cc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL340080 117666 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 438 7 2 3 5.7 N#Cc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
10917990 16501 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 491 7 2 5 5.7 COc1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL123580 16501 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 491 7 2 5 5.7 COc1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
11729258 16852 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 409 8 0 3 5.1 N#CC(CCCN1CCN(Cc2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL124808 16852 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 409 8 0 3 5.1 N#CC(CCCN1CCN(Cc2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44419323 84169 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 390 8 3 3 4.5 N#Cc1cccc(NC(=O)NCCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220800 84169 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 390 8 3 3 4.5 N#Cc1cccc(NC(=O)NCCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
11609863 16853 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 343 6 1 2 4.6 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccccc2)CC1 10.1021/jm0201767
CHEMBL124813 16853 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 343 6 1 2 4.6 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccccc2)CC1 10.1021/jm0201767
44390851 123926 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NC[C@H]2CCCN(CCCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL362613 123926 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NC[C@H]2CCCN(CCCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
44442599 93702 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93702 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
44295145 191706 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 502 5 2 3 4.0 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)Nc1ccc(I)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51953 191706 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 502 5 2 3 4.0 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)Nc1ccc(I)cc1 10.1016/s0960-894x(02)00206-8
11059385 158489 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 448 8 1 2 5.6 O=C(Cc1ccc(F)cc1)Nc1ccccc1CCN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL409001 158489 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 448 8 1 2 5.6 O=C(Cc1ccc(F)cc1)Nc1ccccc1CCN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44440419 93584 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 603 8 0 6 5.6 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(C#N)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246346 93584 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 603 8 0 6 5.6 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(C#N)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440393 93969 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 586 10 0 5 6.8 Cc1c(CN(CCCCc2ccccc2)C2CCN(C(=O)c3cccc4ccccc34)CC2)c(=O)n(-c2ccccc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL248178 93969 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 586 10 0 5 6.8 Cc1c(CN(CCCCc2ccccc2)C2CCN(C(=O)c3cccc4ccccc34)CC2)c(=O)n(-c2ccccc2)n1C 10.1016/j.bmcl.2007.05.035
44445851 154671 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 573 7 2 7 5.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)OC(C)(C)C)C[C@@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL399133 154671 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 573 7 2 7 5.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)OC(C)(C)C)C[C@@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44295354 189270 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 8 2 3 4.2 CN(C)c1ccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51110 189270 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 8 2 3 4.2 CN(C)c1ccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
23509664 196489 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 421 6 1 3 4.9 COc1cccc(NC(=O)N2CCC(CN3CCC(Cc4ccccc4)CC3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL54251 196489 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 421 6 1 3 4.9 COc1cccc(NC(=O)N2CCC(CN3CCC(Cc4ccccc4)CC3)CC2)c1 10.1016/s0960-894x(02)00206-8
9907041 167932 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 363 7 2 5 2.2 CCOC(=O)[C@H](Cc1ccc(O)cc1)NS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(01)00248-7
CHEMBL430745 167932 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 363 7 2 5 2.2 CCOC(=O)[C@H](Cc1ccc(O)cc1)NS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(01)00248-7
10974378 114361 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 664 12 3 4 7.4 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL333063 114361 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 664 12 3 4 7.4 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
71458114 79647 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 4.9 CC(=O)c1cccc(NC(=O)NCCCN2CC3CCC2[C@@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
CHEMBL2114958 79647 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 4.9 CC(=O)c1cccc(NC(=O)NCCCN2CC3CCC2[C@@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
10983419 117525 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 461 7 3 3 5.6 O=C(Nc1ccccc1)Nc1cccc(C(=O)O)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL339884 117525 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 461 7 3 3 5.6 O=C(Nc1ccccc1)Nc1cccc(C(=O)O)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44295480 189719 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 439 6 1 3 5.2 COc1cccc(NC(=O)N2CCCCC2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51480 189719 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 439 6 1 3 5.2 COc1cccc(NC(=O)N2CCCCC2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
20613253 113405 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 446 7 1 2 6.4 Cc1ccc(C(=O)NC(CC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
CHEMBL331702 113405 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 446 7 1 2 6.4 Cc1ccc(C(=O)NC(CC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
44281525 109759 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 314 6 2 5 1.7 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)c1ccccn1 10.1016/s0960-894x(01)00248-7
CHEMBL32282 109759 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 314 6 2 5 1.7 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)c1ccccn1 10.1016/s0960-894x(01)00248-7
10928228 16802 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 435 6 2 2 6.1 O=C(Nc1cc(F)ccc1F)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL124583 16802 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 435 6 2 2 6.1 O=C(Nc1cc(F)ccc1F)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
10874167 170945 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 457 7 2 4 5.2 O=C(NCc1ccc2c(c1)OCO2)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL445379 170945 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 457 7 2 4 5.2 O=C(NCc1ccc2c(c1)OCO2)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
44281789 111413 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 454 8 1 5 4.8 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)OCc1ccccc1)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL32692 111413 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 454 8 1 5 4.8 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)OCc1ccccc1)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11026634 113394 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 443 8 2 3 5.8 COc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL331634 113394 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 443 8 2 3 5.8 COc1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
22022826 16456 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 472 7 1 2 6.5 Cc1ccc(C(=O)NC(CN2C3CCC2CC(Cc2ccc(Cl)c(Cl)c2)C3)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
CHEMBL123308 16456 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 472 7 1 2 6.5 Cc1ccc(C(=O)NC(CN2C3CCC2CC(Cc2ccc(Cl)c(Cl)c2)C3)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
44419322 84408 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 362 6 3 3 3.7 N#Cc1cccc(NC(=O)NCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL221901 84408 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 362 6 3 3 3.7 N#Cc1cccc(NC(=O)NCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
15907328 163458 None 22 Human Binding pIC50 = 4.7 4.7 - 0
Evaluated for its inhibitory activity against human Chemokine receptor type 3 expressed in chinese hamster ovary cellsEvaluated for its inhibitory activity against human Chemokine receptor type 3 expressed in chinese hamster ovary cells
ChEMBL 301 3 1 2 3.8 OC1(c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL419244 163458 None 22 Human Binding pIC50 = 4.7 4.7 - 0
Evaluated for its inhibitory activity against human Chemokine receptor type 3 expressed in chinese hamster ovary cellsEvaluated for its inhibitory activity against human Chemokine receptor type 3 expressed in chinese hamster ovary cells
ChEMBL 301 3 1 2 3.8 OC1(c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm0201767
44447374 94782 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 499 11 4 8 2.2 CCN(C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](C)[C@@H](O)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
CHEMBL253034 94782 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 499 11 4 8 2.2 CCN(C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](C)[C@@H](O)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
44289763 165146 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 412 7 2 3 4.3 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccc(F)cc3F)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42264 165146 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 412 7 2 3 4.3 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccc(F)cc3F)C2)c1 10.1016/j.bmcl.2004.01.059
22143196 184093 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of CCR3 at 10 uMInhibition of CCR3 at 10 uM
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 184093 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of CCR3 at 10 uMInhibition of CCR3 at 10 uM
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
209394 116696 None 9 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 297 6 1 3 2.6 CCOC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL33693 116696 None 9 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 297 6 1 3 2.6 CCOC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
11814253 117019 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cccc(C(F)(F)F)c1 10.1021/jm0201767
CHEMBL338624 117019 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cccc(C(F)(F)F)c1 10.1021/jm0201767
12000105 84276 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 453 10 2 3 5.7 CCCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL221067 84276 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 453 10 2 3 5.7 CCCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
11227406 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm300682j
CHEMBL250689 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm300682j
11272103 124442 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2008.11.002
CHEMBL363840 124442 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2008.11.002
44445876 94140 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 501 7 2 6 4.2 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249060 94140 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 501 7 2 6 4.2 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445856 94316 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 557 8 2 6 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL250262 94316 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 557 8 2 6 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11227406 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL250689 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
44445892 94474 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CC(=O)N(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251045 94474 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 572 9 2 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CC(=O)N(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445840 94504 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 488 7 2 6 4.3 CC(=O)c1sc(NC(=O)N[C@@H]2CCOC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251232 94504 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 488 7 2 6 4.3 CC(=O)c1sc(NC(=O)N[C@@H]2CCOC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445894 154821 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 612 8 2 7 4.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C3CCN(C(C)=O)CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL399893 154821 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 612 8 2 7 4.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C3CCN(C(C)=O)CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
21362425 155093 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 584 8 2 7 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C3CCN(C)CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL401394 155093 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 584 8 2 7 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C3CCN(C)CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11227406 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL250689 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
44455509 166521 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 493 9 2 6 4.4 CCc1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL427728 166521 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 493 9 2 6 4.4 CCc1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455560 169382 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 517 9 2 8 3.8 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2ccnn2)cc(-n2ccnn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL441334 169382 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 517 9 2 8 3.8 C[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2ccnn2)cc(-n2ccnn2)c1 10.1016/j.bmcl.2007.11.067
11363006 70459 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
CHEMBL194601 70459 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1 10.1021/jm049530m
11227406 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL250689 94398 None 2 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44401123 136365 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 516 7 2 5 4.9 N#CC1=CC(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)CC=C1n1cccn1 10.1021/jm049530m
CHEMBL373347 136365 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 516 7 2 5 4.9 N#CC1=CC(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)CC=C1n1cccn1 10.1021/jm049530m
11017618 11474 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 501 6 2 4 5.7 C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL1180385 11474 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 501 6 2 4 5.7 C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL124689 11474 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 501 6 2 4 5.7 C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
11762511 16570 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 474 7 3 3 5.3 CNC(=O)c1cccc(NC(=O)Nc2ccccc2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL123837 16570 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 474 7 3 3 5.3 CNC(=O)c1cccc(NC(=O)Nc2ccccc2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
11134936 16752 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 504 8 3 4 5.3 CNC(=O)c1cccc(NC(=O)Nc2cccc(OC)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL124334 16752 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 504 8 3 4 5.3 CNC(=O)c1cccc(NC(=O)Nc2cccc(OC)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
11038430 16830 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 502 8 3 4 5.2 CC(=O)c1cccc(NC(=O)Nc2cccc(C(N)=O)c2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL124722 16830 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 502 8 3 4 5.2 CC(=O)c1cccc(NC(=O)Nc2cccc(C(N)=O)c2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44570581 178521 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 536 10 2 8 3.1 CN1C[C@@H](NC(=O)Nc2cccc(-c3nnnn3C)c2)[C@H](CN(CCCc2ccc(F)cc2)C2CC2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL465942 178521 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 536 10 2 8 3.1 CN1C[C@@H](NC(=O)Nc2cccc(-c3nnnn3C)c2)[C@H](CN(CCCc2ccc(F)cc2)C2CC2)OC1=O 10.1016/j.bmcl.2008.11.002
44445847 94477 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CNCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251079 94477 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 487 7 3 6 3.8 CC(=O)c1sc(NC(=O)N[C@@H]2CNCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445878 154688 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 557 8 2 6 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL399150 154688 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 557 8 2 6 4.7 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445880 155326 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 8 2 6 4.5 CCC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL402707 155326 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 8 2 6 4.5 CCC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
21362416 94137 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 612 8 2 7 4.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C3CCN(C(C)=O)CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249058 94137 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 612 8 2 7 4.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C3CCN(C(C)=O)CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390927 63020 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 493 9 2 6 4.3 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2CC)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL178671 63020 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 493 9 2 6 4.3 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2CC)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44390894 122426 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 9 2 6 4.0 CCc1cc(NC(=O)NC[C@H]2CCCN(CCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL360039 122426 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 9 2 6 4.0 CCc1cc(NC(=O)NC[C@H]2CCCN(CCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
11179351 124681 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 490 7 2 5 5.0 O=C(Nc1ccc(-n2cncn2)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL364068 124681 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 490 7 2 5 5.0 O=C(Nc1ccc(-n2cncn2)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44419300 84037 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 499 11 2 4 5.4 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCF)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220713 84037 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 499 11 2 4 5.4 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCF)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
795 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(03)00748-0
796 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(03)00748-0
9913085 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(03)00748-0
CHEMBL20921 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(03)00748-0
795 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
796 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
9913085 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
CHEMBL20921 574 None 5 Human Binding pIC50 = 8.6 8.6 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
44445875 94138 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 531 9 3 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CCO)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249059 94138 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 531 9 3 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CCO)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445859 154876 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 545 7 2 7 4.3 COC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL400173 154876 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 545 7 2 7 4.3 COC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
44401561 124188 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL363373 124188 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 463 6 3 3 5.3 O=C(Nc1ccc2[nH]ncc2c1)N[C@@H]1CCCC[C@H]1CN1CCCC(Cc2ccc(F)cc2)C1 10.1021/jm049530m
11750808 126264 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 431 6 2 5 4.3 O=C(Nc1nncs1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL364977 126264 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 431 6 2 5 4.3 O=C(Nc1nncs1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44346210 168058 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 531 10 3 6 4.7 COc1cc(NC(=O)N[C@@H](CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)[C@H](C)O)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
CHEMBL431670 168058 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 531 10 3 6 4.7 COc1cc(NC(=O)N[C@@H](CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)[C@H](C)O)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
44455845 97512 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 537 10 3 7 4.5 CC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL270146 97512 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 537 10 3 7 4.5 CC[C@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2nnnn2C)cc(C(C)(C)O)c1 10.1016/j.bmcl.2007.11.067
44289713 166203 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 527 9 2 6 5.2 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42599 166203 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 527 9 2 6 5.2 Cn1nnnc1-c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.059
44419335 84175 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 465 10 2 3 5.7 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC2CC2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220819 84175 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 465 10 2 3 5.7 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC2CC2)c1 10.1016/j.bmcl.2006.08.012
44447140 94607 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 523 11 3 7 4.2 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)C1CCCCC1 10.1016/j.bmcl.2007.11.087
CHEMBL251839 94607 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 523 11 3 7 4.2 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)C1CCCCC1 10.1016/j.bmcl.2007.11.087
44447154 94745 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 559 13 3 7 4.6 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)Cc2ccccc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL252792 94745 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 559 13 3 7 4.6 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)Cc2ccccc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447380 94943 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 483 11 3 7 3.2 CCN(C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](C)CCc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
CHEMBL254093 94943 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 483 11 3 7 3.2 CCN(C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](C)CCc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
44445907 94886 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 409 7 2 3 4.6 CC(=O)c1cccc(NC(=O)N/C=C/CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL253676 94886 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 409 7 2 3 4.6 CC(=O)c1cccc(NC(=O)N/C=C/CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
44445883 155327 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 555 8 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C3CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL402708 155327 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 555 8 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C3CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44290039 178907 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL46905 178907 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.11.067
11430170 123900 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 423 6 2 2 5.5 O=C(Nc1ccccc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL362466 123900 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 423 6 2 2 5.5 O=C(Nc1ccccc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11385766 132864 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL370082 132864 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44290039 178907 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL46905 178907 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44290039 178907 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL46905 178907 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44445849 94505 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 573 7 2 7 5.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)OC(C)(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251243 94505 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 573 7 2 7 5.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)OC(C)(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445889 154956 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 567 9 2 7 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CN(Cc3ccco3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL400649 154956 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 567 9 2 7 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CN(Cc3ccco3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44289919 101207 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 493 9 2 7 3.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL295415 101207 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 493 9 2 7 3.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455683 155178 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 531 9 3 7 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL401879 155178 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 531 9 3 7 4.4 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-n2cccn2)cc(-n2cccn2)c1 10.1016/j.bmcl.2007.11.067
44455485 155588 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 507 9 2 6 5.0 CC(C)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL404122 155588 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 507 9 2 6 5.0 CC(C)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44455484 167502 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 493 9 2 6 4.6 CC(C)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL429604 167502 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 493 9 2 6 4.6 CC(C)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
44387842 131369 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 369 5 2 3 4.2 CC(=O)c1cccc(NC(=O)NN2CCCCC2Cc2ccc(F)cc2)c1 10.1021/jm049530m
CHEMBL368683 131369 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 369 5 2 3 4.2 CC(=O)c1cccc(NC(=O)NN2CCCCC2Cc2ccc(F)cc2)c1 10.1021/jm049530m
10457573 117112 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 473 8 2 3 6.2 CC(=O)c1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL339110 117112 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 473 8 2 3 6.2 CC(=O)c1cccc(NC(=O)Nc2ccccc2CCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44289919 101207 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 493 9 2 7 3.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
CHEMBL295415 101207 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 493 9 2 7 3.7 CC(=O)c1cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.01.059
44445893 154501 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 541 9 2 6 5.0 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CC3CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL398889 154501 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 541 9 2 6 5.0 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CC3CC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455459 95144 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL255398 95144 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
44455460 95145 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 533 9 3 7 5.3 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2ncco2)cc(-c2ncco2)c1 10.1016/j.bmcl.2007.11.067
CHEMBL255399 95145 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 533 9 3 7 5.3 C[C@H](C[C@@H](O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cc(-c2ncco2)cc(-c2ncco2)c1 10.1016/j.bmcl.2007.11.067
44455767 95774 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 483 9 3 5 4.4 CC(=O)c1cc(NC(=O)N[C@@H](C)C[C@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL258309 95774 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 483 9 3 5 4.4 CC(=O)c1cc(NC(=O)N[C@@H](C)C[C@H](O)N2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
11487192 69697 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 428 6 2 4 4.8 Cc1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)no1 10.1021/jm049530m
CHEMBL193526 69697 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 428 6 2 4 4.8 Cc1cc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)no1 10.1021/jm049530m
44445896 154626 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 531 9 3 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CCO)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL399088 154626 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 531 9 3 7 3.6 CC(=O)c1sc(NC(=O)N[C@@H]2CN(CCO)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445855 154875 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 583 8 2 6 5.3 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C3CCCC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL400172 154875 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 583 8 2 6 5.3 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C3CCCC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11113940 79613 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 509 8 1 6 5.9 CCOc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 10.1016/s0960-894x(01)00176-7
CHEMBL21143 79613 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 509 8 1 6 5.9 CCOc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 10.1016/s0960-894x(01)00176-7
44440402 93970 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL248179 93970 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44295648 102055 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 9 3 4 4.1 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@H](C)O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL301601 102055 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 9 3 4 4.1 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@H](C)O)c1 10.1016/s0960-894x(02)00206-8
44295555 102109 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 447 8 2 4 3.7 CS(=O)(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL301974 102109 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 447 8 2 4 3.7 CS(=O)(=O)c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
22393430 168805 None 0 Human Binding pIC50 = 7.7 7.7 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL43677 168805 None 0 Human Binding pIC50 = 7.7 7.7 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
22393339 186842 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 410 7 2 3 4.7 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(Cl)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL48873 186842 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 410 7 2 3 4.7 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(Cl)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44295306 188991 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 415 8 2 3 5.0 CSc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50726 188991 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 415 8 2 3 5.0 CSc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
22393469 189483 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 7 2 3 4.2 N#Cc1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51286 189483 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 7 2 3 4.2 N#Cc1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
44295566 194826 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 11 3 4 5.1 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@@H](O)CC(C)C)c1 10.1016/s0960-894x(02)00206-8
CHEMBL53444 194826 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 11 3 4 5.1 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@@H](O)CC(C)C)c1 10.1016/s0960-894x(02)00206-8
22393430 168805 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43677 168805 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
44440429 93696 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 580 8 0 5 5.4 Cc1c(CN(CCc2ccc(F)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246768 93696 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 580 8 0 5 5.4 Cc1c(CN(CCc2ccc(F)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440445 146835 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 577 8 0 6 4.3 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3cccc[n+]3[O-])CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL392430 146835 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 577 8 0 6 4.3 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3cccc[n+]3[O-])CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44295674 101688 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 483 10 2 3 6.0 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2Cc2ccccc2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL298999 101688 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 483 10 2 3 6.0 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2Cc2ccccc2)c1 10.1016/s0960-894x(02)00206-8
22393362 101744 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 7 2 2 5.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00206-8
CHEMBL299385 101744 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 7 2 2 5.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00206-8
9842640 167470 None 0 Human Binding pIC50 = 6.7 6.7 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 376 7 2 3 4.0 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL42948 167470 None 0 Human Binding pIC50 = 6.7 6.7 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 376 7 2 3 4.0 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44295267 188339 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 431 8 2 3 4.0 C[S+]([O-])c1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL49938 188339 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 431 8 2 3 4.0 C[S+]([O-])c1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
44295406 188471 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 8 2 3 6.0 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(-c2cccs2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50129 188471 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 8 2 3 6.0 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(-c2cccs2)c1 10.1016/s0960-894x(02)00206-8
44295664 188802 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 10 2 3 5.5 CCC[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50423 188802 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 435 10 2 3 5.5 CCC[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
22393307 188879 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3F)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50557 188879 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3F)CC2)c1 10.1016/s0960-894x(02)00206-8
44295304 189237 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 9 3 4 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2C(C)(C)O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51052 189237 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 9 3 4 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2C(C)(C)O)c1 10.1016/s0960-894x(02)00206-8
22393366 192629 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 411 8 2 3 4.5 CC(=O)c1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL52094 192629 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 411 8 2 3 4.5 CC(=O)c1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
9842640 167470 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 376 7 2 3 4.0 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42948 167470 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 376 7 2 3 4.0 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2004.01.059
44349614 118514 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 402 5 0 3 3.6 O=C1CC2(CCc3ccccc32)C(=O)N1CC1CCN(CCc2ccccc2)CC1 10.1021/jm0201767
CHEMBL341144 118514 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 402 5 0 3 3.6 O=C1CC2(CCc3ccccc32)C(=O)N1CC1CCN(CCc2ccccc2)CC1 10.1021/jm0201767
44281791 116335 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 406 7 1 5 4.0 CC(C)OC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33589 116335 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 406 7 1 5 4.0 CC(C)OC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11103845 12130 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 455 6 3 3 5.5 C[N+]1(Cc2cc(O)ccc2NC(=O)Nc2cccc(C#N)c2)CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL1184106 12130 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 455 6 3 3 5.5 C[N+]1(Cc2cc(O)ccc2NC(=O)Nc2cccc(C#N)c2)CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL332591 12130 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 455 6 3 3 5.5 C[N+]1(Cc2cc(O)ccc2NC(=O)Nc2cccc(C#N)c2)CCC(Cc2ccccc2)CC1 10.1021/jm0201767
11812807 16585 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 477 8 3 4 5.5 COc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL123917 16585 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 477 8 3 4 5.5 COc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44447161 94937 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 547 12 3 8 2.3 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)S(C)(=O)=O)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254055 94937 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 547 12 3 8 2.3 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)S(C)(=O)=O)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44447153 154021 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 617 13 3 7 5.6 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC23CC4CC(CC(C4)C2)C3)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL398344 154021 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 617 13 3 7 5.6 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC23CC4CC(CC(C4)C2)C3)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44419314 83333 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218997 83333 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
11828215 114523 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 613 12 3 3 7.1 O=C(NCCc1ccc(F)cc1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL333422 114523 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 613 12 3 3 7.1 O=C(NCCc1ccc(F)cc1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11104005 117424 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 602 12 3 4 6.2 O=C(NCCN1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL339752 117424 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 602 12 3 4 6.2 O=C(NCCN1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11813735 118209 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 562 12 3 4 5.3 CN(C)CCNC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL340797 118209 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 562 12 3 4 5.3 CN(C)CCNC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11730610 16692 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 485 7 2 5 5.7 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccccc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL124272 16692 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 485 7 2 5 5.7 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccccc4)CC2)OCO3)c1 10.1021/jm0201767
44390949 64426 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCC2CCN(CCCc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL181311 64426 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCC2CCN(CCCc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.11.006
44512617 197794 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibition of mouse CCR3Inhibition of mouse CCR3
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
CHEMBL551735 197794 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibition of mouse CCR3Inhibition of mouse CCR3
ChEMBL 487 5 2 4 4.2 O=C(C=C1CCN(C(=O)c2ccccc2O)CC1)N[C@@H]1CCN(Cc2ccc3cc(F)ccc3c2)C1 10.1016/j.bmc.2009.06.066
44295686 163096 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 407 5 1 3 4.6 COc1cccc(NC(=O)N2CCC(N3CCC(Cc4ccccc4)CC3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL417547 163096 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 407 5 1 3 4.6 COc1cccc(NC(=O)N2CCC(N3CCC(Cc4ccccc4)CC3)CC2)c1 10.1016/s0960-894x(02)00206-8
10995218 16623 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 549 12 4 4 5.1 O=C(NCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL124127 16623 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 549 12 4 4 5.1 O=C(NCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
9982077 16594 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 468 6 2 5 5.4 N#Cc1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccccc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL123962 16594 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 468 6 2 5 5.4 N#Cc1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccccc4)CC2)OCO3)c1 10.1021/jm0201767
44447373 94728 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(C)[C@H](C)[C@@H](O)c1ccccc1 10.1016/j.bmcl.2007.11.087
CHEMBL252628 94728 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(C)[C@H](C)[C@@H](O)c1ccccc1 10.1016/j.bmcl.2007.11.087
10863252 171459 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 447 7 3 3 5.5 O=C(Nc1ccccc1)Nc1ccccc1C(O)CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL446164 171459 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 447 7 3 3 5.5 O=C(Nc1ccccc1)Nc1ccccc1C(O)CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44295479 101611 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 425 6 1 3 4.6 COc1cccc(NC(=O)N2CCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL298414 101611 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 425 6 1 3 4.6 COc1cccc(NC(=O)N2CCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
11285792 879 None 32 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from CCR3 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 879 None 32 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from CCR3 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 879 None 32 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from CCR3 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 879 None 32 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from CCR3 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
10983106 16936 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 443 8 2 3 5.5 COc1cccc(NC(=O)NCc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL125282 16936 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 443 8 2 3 5.5 COc1cccc(NC(=O)NCc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
11124782 118533 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 587 11 3 3 7.3 O=C(NCC1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL341306 118533 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 587 11 3 3 7.3 O=C(NCC1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
22393396 168373 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3cccc(F)c3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43391 168373 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3cccc(F)c3)C2)c1 10.1016/j.bmcl.2004.01.059
11732727 16657 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 429 7 3 3 5.3 O=C(Nc1ccccc1)Nc1ccccc1C(O)CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL124206 16657 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 429 7 3 3 5.3 O=C(Nc1ccccc1)Nc1ccccc1C(O)CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
44440396 153156 None 1 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 579 8 0 6 5.2 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccccn2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL397599 153156 None 1 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 579 8 0 6 5.2 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccccn2)n1C 10.1016/j.bmcl.2007.05.035
44440427 93695 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 609 9 0 7 5.2 COc1ccncc1-n1c(=O)c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(C)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246766 93695 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 609 9 0 7 5.2 COc1ccncc1-n1c(=O)c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(C)n1C 10.1016/j.bmcl.2007.05.035
44295499 189466 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 453 7 1 3 5.4 COc1cccc(NC(=O)N2CCCC(CCN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51267 189466 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 453 7 1 3 5.4 COc1cccc(NC(=O)N2CCCC(CCN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44440422 93586 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 622 9 1 6 5.5 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(C(=O)O)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246348 93586 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 622 9 1 6 5.5 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(C(=O)O)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440440 93697 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 577 8 1 6 4.8 Cc1c(CN(CCc2ccc(N)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246769 93697 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 577 8 1 6 4.8 Cc1c(CN(CCc2ccc(N)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44440434 153452 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 563 8 0 6 4.6 Cc1c(CN(CCc2cccnc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL397853 153452 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 563 8 0 6 4.6 Cc1c(CN(CCc2cccnc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44295409 101719 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 355 5 1 3 3.2 CC(C)(C)C(=O)NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3 10.1016/s0960-894x(02)00206-8
CHEMBL299226 101719 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 355 5 1 3 3.2 CC(C)(C)C(=O)NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3 10.1016/s0960-894x(02)00206-8
44295433 187166 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCO[C@@H](CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL49117 187166 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCO[C@@H](CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
23497297 16881 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 483 6 3 5 5.4 O=C(Nc1ccc2c[nH]nc2c1)Nc1cc2c(cc1CN1CCC(Cc3ccccc3)CC1)OCO2 10.1021/jm0201767
CHEMBL124966 16881 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 483 6 3 5 5.4 O=C(Nc1ccc2c[nH]nc2c1)Nc1cc2c(cc1CN1CCC(Cc3ccccc3)CC1)OCO2 10.1021/jm0201767
11001953 114197 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 327 7 2 4 2.2 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Cc1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL33290 114197 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 327 7 2 4 2.2 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Cc1ccccc1 10.1016/s0960-894x(01)00248-7
11825113 16894 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 381 8 3 3 3.6 O=C(NCCCO)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL125026 16894 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 381 8 3 3 3.6 O=C(NCCCO)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
11762865 16568 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 503 9 2 2 7.1 O=C(NCC(c1ccccc1)c1ccccc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL123807 16568 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 503 9 2 2 7.1 O=C(NCC(c1ccccc1)c1ccccc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
44570714 189903 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCR3 at 10 uMInhibition of CCR3 at 10 uM
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189903 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCR3 at 10 uMInhibition of CCR3 at 10 uM
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
11048458 118542 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 440 6 3 4 5.4 N#Cc1cccc(NC(=O)Nc2ccc(O)cc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL341343 118542 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 440 6 3 4 5.4 N#Cc1cccc(NC(=O)Nc2ccc(O)cc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
71449114 78978 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 435 7 2 3 5.3 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCCC(Cc3ccccc3)C2)c1 10.1021/jm049530m
CHEMBL2112987 78978 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 435 7 2 3 5.3 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCCC(Cc3ccccc3)C2)c1 10.1021/jm049530m
10928173 76570 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.8 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL20612 76570 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.8 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(01)00176-7
10950225 117538 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 438 7 2 3 5.3 N#Cc1cccc(NC(=O)NCc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL339934 117538 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 438 7 2 3 5.3 N#Cc1cccc(NC(=O)NCc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
76316987 103590 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 9 2 6 3.9 Cn1nnnc1-c1cccc(NC(=O)NC[C@@H]2CCCN(CCCCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL3085295 103590 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 9 2 6 3.9 Cn1nnnc1-c1cccc(NC(=O)NC[C@@H]2CCCN(CCCCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
11408397 77988 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL2096695 77988 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
22393329 101180 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL295229 101180 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44390970 64085 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 533 8 2 6 4.4 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2C(F)(F)F)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180728 64085 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 533 8 2 6 4.4 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2C(F)(F)F)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44390971 123188 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 541 9 2 6 5.0 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2c2ccccc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL361130 123188 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 541 9 2 6 5.0 CCc1cc(NC(=O)NC[C@H]2CN(CCc3ccc(F)cc3)CC[C@@H]2c2ccccc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44387856 131510 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 447 7 2 3 5.5 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
CHEMBL369073 131510 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 447 7 2 3 5.5 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
11465468 167133 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL428881 167133 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
44281521 100456 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 370 7 1 5 3.1 CCOC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1ccc(C)cc1C 10.1016/s0960-894x(01)00248-7
CHEMBL290104 100456 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 370 7 1 5 3.1 CCOC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1ccc(C)cc1C 10.1016/s0960-894x(01)00248-7
10255492 118225 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 502 8 3 4 5.2 CC(=O)c1cccc(NC(=O)Nc2ccc(C(N)=O)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL340853 118225 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 502 8 3 4 5.2 CC(=O)c1cccc(NC(=O)Nc2ccc(C(N)=O)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
11733617 161348 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 485 7 3 4 4.9 N#Cc1cccc(NC(=O)Nc2cccc(C(N)=O)c2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL411956 161348 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 485 7 3 4 4.9 N#Cc1cccc(NC(=O)Nc2cccc(C(N)=O)c2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44289910 101265 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 529 8 2 6 4.2 Cn1nnnc1-c1cc(Br)cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL295898 101265 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 529 8 2 6 4.2 Cn1nnnc1-c1cc(Br)cc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44290019 101276 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 479 9 2 6 4.5 CC(C)n1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL295970 101276 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 479 9 2 6 4.5 CC(C)n1nnnc1-c1cccc(NC(=O)NCCCN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44447149 94997 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 551 12 3 7 4.7 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)C2CCCCC2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254470 94997 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 551 12 3 7 4.7 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)C2CCCCC2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44445862 94507 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 555 8 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C3CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251274 94507 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 555 8 2 6 4.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)C3CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390954 63889 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 483 8 2 6 3.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)c(F)c3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180351 63889 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 483 8 2 6 3.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)c(F)c3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44445861 94344 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 8 2 6 4.5 CCC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL250436 94344 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 8 2 6 4.5 CCC(=O)N1CC[C@@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2007.03.065
44447378 154929 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 527 12 4 8 2.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)[C@@H](C)[C@H](O)Cc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL400467 154929 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 527 12 4 8 2.8 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CC)[C@@H](C)[C@H](O)Cc2ccc(F)cc2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44390838 128577 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL366710 128577 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44419299 141777 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 510 11 3 5 3.9 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC(N)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL385607 141777 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 510 11 3 5 3.9 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CC(N)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
11953409 94269 None 0 Mouse Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 mins
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249854 94269 None 0 Mouse Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 mins
ChEMBL 529 7 2 6 4.1 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(C)=O)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44445877 94267 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 583 8 2 6 5.3 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C3CCCC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249851 94267 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 583 8 2 6 5.3 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)C3CCCC3)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390964 62618 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 481 8 2 6 4.2 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(Cl)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL178287 62618 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 481 8 2 6 4.2 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(Cl)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44289877 166136 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 5 4.3 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cccc(-c2nnco2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42562 166136 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 5 4.3 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cccc(-c2nnco2)c1 10.1016/j.bmcl.2004.01.059
11213457 94816 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 465 9 3 6 3.9 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CNCCCc2ccc(F)cc2)c1 10.1016/j.bmcl.2007.11.087
CHEMBL253209 94816 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 465 9 3 6 3.9 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CNCCCc2ccc(F)cc2)c1 10.1016/j.bmcl.2007.11.087
44390919 122119 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 447 8 2 6 3.5 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccccc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL359609 122119 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 447 8 2 6 3.5 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccccc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44419306 141474 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 495 9 2 4 5.0 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL383879 141474 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 495 9 2 4 5.0 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44295434 101623 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCO[C@H](CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL298505 101623 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCO[C@H](CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44295362 162315 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 369 7 2 2 4.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccccc1 10.1016/s0960-894x(02)00206-8
CHEMBL416305 162315 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 369 7 2 2 4.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccccc1 10.1016/s0960-894x(02)00206-8
22393419 165524 None 0 Human Binding pIC50 = 7.5 7.5 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 399 8 2 3 4.3 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL42388 165524 None 0 Human Binding pIC50 = 7.5 7.5 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 399 8 2 3 4.3 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
23509697 196586 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 440 6 2 4 3.6 COc1cccc(NC(=O)N2CCNC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL54273 196586 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 440 6 2 4 3.6 COc1cccc(NC(=O)N2CCNC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
22393419 165524 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 399 8 2 3 4.3 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42388 165524 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 399 8 2 3 4.3 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
9951883 168795 None 0 Human Binding pIC50 = 6.5 6.5 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 381 8 2 3 4.2 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL43666 168795 None 0 Human Binding pIC50 = 6.5 6.5 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 381 8 2 3 4.2 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
22393378 189069 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 397 9 2 2 4.0 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NCCc1ccccc1 10.1016/s0960-894x(02)00206-8
CHEMBL50829 189069 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 397 9 2 2 4.0 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NCCc1ccccc1 10.1016/s0960-894x(02)00206-8
9951883 168795 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 381 8 2 3 4.2 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43666 168795 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 381 8 2 3 4.2 COc1cccc(NC(=O)NCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2004.01.059
11734303 168680 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 547 9 3 3 6.5 CC(C)(C)NC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL435812 168680 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 547 9 3 3 6.5 CC(C)(C)NC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11396966 79036 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 457 6 2 2 6.1 O=C(Nc1cccc(Cl)c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL2113082 79036 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 457 6 2 2 6.1 O=C(Nc1cccc(Cl)c1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44289762 166030 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 380 7 2 3 3.8 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL42507 166030 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 380 7 2 3 3.8 N#Cc1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
11059280 116969 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 442 6 2 3 5.8 N#Cc1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL338389 116969 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 442 6 2 3 5.8 N#Cc1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
11037958 75998 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm300682j
CHEMBL20532 75998 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm300682j
11037958 75998 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL20532 75998 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(01)00176-7
44440394 93776 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 578 8 0 5 5.8 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccccc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL247160 93776 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 578 8 0 5 5.8 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccccc2)n1C 10.1016/j.bmcl.2007.05.035
9927733 116964 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 336 6 2 3 3.1 CCOC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL33838 116964 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 336 6 2 3 3.1 CCOC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
9888454 101934 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 421 6 1 3 4.9 COc1cccc(NC(=O)N2CCCC(CN3CCC(Cc4ccccc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL300726 101934 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 421 6 1 3 4.9 COc1cccc(NC(=O)N2CCCC(CN3CCC(Cc4ccccc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44281522 111575 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 391 6 1 4 3.2 CN(C)C(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL32784 111575 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 391 6 1 4 3.2 CN(C)C(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11133428 16735 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 413 7 2 2 5.5 O=C(NCc1ccccc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL124321 16735 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 413 7 2 2 5.5 O=C(NCc1ccccc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
10863284 18565 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 449 7 2 2 6.1 O=C(Nc1ccc(F)cc1)Nc1ccccc1CCN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL127590 18565 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 449 7 2 2 6.1 O=C(Nc1ccc(F)cc1)Nc1ccccc1CCN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44390931 122998 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NCC2CCN(CCc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL360653 122998 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NCC2CCN(CCc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.11.006
76320703 103591 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 423 6 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NC[C@@H]2CCCN(Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL3085296 103591 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 423 6 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NC[C@@H]2CCCN(Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
10875472 113723 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 568 10 3 4 6.6 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccncc1 10.1021/jm0201767
CHEMBL332277 113723 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 568 10 3 4 6.6 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccncc1 10.1021/jm0201767
9981262 64876 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCC2CCCN(CCCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL182087 64876 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCC2CCCN(CCCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
10874195 164451 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 459 8 3 4 5.3 COc1cccc(NC(=O)Nc2cc(CO)ccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL421273 164451 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 459 8 3 4 5.3 COc1cccc(NC(=O)Nc2cc(CO)ccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
11112528 16820 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 417 6 2 2 5.9 O=C(Nc1ccccc1)Nc1ccccc1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL124669 16820 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 417 6 2 2 5.9 O=C(Nc1ccccc1)Nc1ccccc1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44295487 169266 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 444 5 2 3 4.5 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)Nc1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL440477 169266 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 444 5 2 3 4.5 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)Nc1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(02)00206-8
11145481 113632 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 496 8 2 3 5.9 O=C(Nc1cccc(CN2CCC(Cc3ccccc3)CC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL332227 113632 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 496 8 2 3 5.9 O=C(Nc1cccc(CN2CCC(Cc3ccccc3)CC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
22393395 168968 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccccc3F)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43818 168968 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 394 7 2 3 4.2 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccccc3F)C2)c1 10.1016/j.bmcl.2004.01.059
44390857 63651 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 490 9 2 7 3.6 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(N(C)C)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180082 63651 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 490 9 2 7 3.6 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(N(C)C)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
10939210 16917 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 445 8 2 2 5.6 O=C(NCCc1ccc(F)cc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL125167 16917 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 445 8 2 2 5.6 O=C(NCCc1ccc(F)cc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
11722772 98638 None 0 Human Binding pIC50 = 5.4 5.4 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 307 7 0 1 5.0 c1ccc(CCCCN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
CHEMBL276784 98638 None 0 Human Binding pIC50 = 5.4 5.4 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 307 7 0 1 5.0 c1ccc(CCCCN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
77033 113859 None 47 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 313 6 2 4 2.3 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL33242 113859 None 47 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 313 6 2 4 2.3 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
22966052 84258 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220866 84258 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
44289959 100473 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 5.0 CC(=O)c1cccc(NC(=O)NCCCN2CC3(Cc4ccc(F)cc4)CCC2CC3)c1 10.1016/j.bmcl.2004.01.059
CHEMBL290276 100473 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 5.0 CC(=O)c1cccc(NC(=O)NCCCN2CC3(Cc4ccc(F)cc4)CCC2CC3)c1 10.1016/j.bmcl.2004.01.059
44290040 172568 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL44817 172568 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 411 8 2 3 4.5 CC(=O)c1cccc(NC(=O)NCCCN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.01.059
44295259 162650 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 393 6 1 3 3.6 O=C(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL416835 162650 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 393 6 1 3 3.6 O=C(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
9935588 16907 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 496 8 2 3 5.9 O=C(Nc1ccccc1CN1CCC(Cc2ccccc2)CC1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL125108 16907 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 496 8 2 3 5.9 O=C(Nc1ccccc1CN1CCC(Cc2ccccc2)CC1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
10874991 164453 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 517 9 2 3 6.7 O=C(NCC(c1ccccc1)c1ccccc1)Nc1ccccc1CN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm0201767
CHEMBL421274 164453 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 517 9 2 3 6.7 O=C(NCC(c1ccccc1)c1ccccc1)Nc1ccccc1CN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm0201767
44445874 94567 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 541 9 2 6 5.0 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CC3CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251623 94567 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 541 9 2 6 5.0 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(CC3CC3)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44455792 95776 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 8 2 6 3.9 C[C@@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL258323 95776 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 465 8 2 6 3.9 C[C@@H](CCN1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
11214474 71377 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 514 6 2 4 6.7 O=C(Nc1nc2c(Cl)cccc2s1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL195790 71377 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 514 6 2 4 6.7 O=C(Nc1nc2c(Cl)cccc2s1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
11442439 124124 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 455 6 2 2 5.9 Cc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1F 10.1021/jm049530m
CHEMBL363166 124124 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 455 6 2 2 5.9 Cc1ccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc1F 10.1021/jm049530m
9804542 130352 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
CHEMBL367992 130352 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm049530m
44419340 84409 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 451 10 2 3 5.4 C=CCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL221903 84409 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 451 10 2 3 5.4 C=CCN1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
10140602 166713 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 7 2 6 3.4 C[C@H](CC(=O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
CHEMBL428071 166713 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 479 7 2 6 3.4 C[C@H](CC(=O)N1CCC[C@@H](Cc2ccc(F)cc2)C1)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.067
20636465 84123 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 495 9 4 4 4.3 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2C(=N)N)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220766 84123 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 495 9 4 4 4.3 CC(=O)c1cc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2C(=N)N)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44346153 15510 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 519 8 3 5 4.1 C[C@H](O)[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
CHEMBL121637 15510 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 519 8 3 5 4.1 C[C@H](O)[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
11259591 125590 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 455 6 2 2 5.9 Cc1ccc(F)cc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL364673 125590 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 455 6 2 2 5.9 Cc1ccc(F)cc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44346194 15555 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 501 9 2 5 5.4 COc1cc(NC(=O)N[C@H](C)CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
CHEMBL121905 15555 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Compound was tested for its ability to inhibit C-C chemokine receptor type 3 receptorCompound was tested for its ability to inhibit C-C chemokine receptor type 3 receptor
ChEMBL 501 9 2 5 5.4 COc1cc(NC(=O)N[C@H](C)CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
44445879 94268 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 545 7 2 7 4.3 COC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL249852 94268 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 545 7 2 7 4.3 COC(=O)N1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
44440412 151110 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccccc2F)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL395850 151110 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 596 8 0 5 5.9 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccccc2F)n1C 10.1016/j.bmcl.2007.05.035
44295554 188451 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 415 8 2 3 5.0 CSc1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL50094 188451 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 415 8 2 3 5.0 CSc1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
23509693 191602 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 540 6 1 5 5.2 COc1cccc(NC(=O)N2CCN(C(=O)OC(C)(C)C)C(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51937 191602 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 540 6 1 5 5.2 COc1cccc(NC(=O)N2CCN(C(=O)OC(C)(C)C)C(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
10029075 116896 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 503 7 2 5 5.9 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL337990 116896 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 503 7 2 5 5.9 CC(=O)c1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
44440423 146798 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 635 9 1 6 5.7 CC(=O)Nc1ccc(-n2c(=O)c(CN(CCc3ccc(Cl)cc3)C3CCN(C(=O)c4c(F)cccc4F)CC3)c(C)n2C)cc1 10.1016/j.bmcl.2007.05.035
CHEMBL392405 146798 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 635 9 1 6 5.7 CC(=O)Nc1ccc(-n2c(=O)c(CN(CCc3ccc(Cl)cc3)C3CCN(C(=O)c4c(F)cccc4F)CC3)c(C)n2C)cc1 10.1016/j.bmcl.2007.05.035
22393428 188761 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 383 8 2 2 4.0 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NCc1ccccc1 10.1016/s0960-894x(02)00206-8
CHEMBL50354 188761 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 383 8 2 2 4.0 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NCc1ccccc1 10.1016/s0960-894x(02)00206-8
22393333 189513 None 2 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 351 7 2 2 4.2 O=C(NCCCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1 10.1016/s0960-894x(02)00206-8
CHEMBL51307 189513 None 2 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 351 7 2 2 4.2 O=C(NCCCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1 10.1016/s0960-894x(02)00206-8
44281523 99742 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 453 8 2 4 4.4 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)NCc1ccccc1)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL284577 99742 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 453 8 2 4 4.4 O=C(N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)NCc1ccccc1)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11282712 78566 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)NC2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1021/jm049530m
CHEMBL2112049 78566 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)NC2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1021/jm049530m
22393315 168785 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 376 7 2 3 4.0 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43655 168785 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 376 7 2 3 4.0 N#Cc1cccc(NC(=O)NCCCN2CCCC(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2004.01.059
11134412 164736 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 465 7 3 3 5.6 O=C(Nc1cc(F)ccc1F)Nc1ccccc1C(O)CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL421634 164736 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 465 7 3 3 5.6 O=C(Nc1cc(F)ccc1F)Nc1ccccc1C(O)CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
10864223 16892 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 517 8 2 5 5.9 COC(=O)c1ccc(NC(=O)Nc2cccc(C(C)=O)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL125012 16892 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 517 8 2 5 5.9 COC(=O)c1ccc(NC(=O)Nc2cccc(C(C)=O)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44447142 94723 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 589 12 3 7 5.0 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)CC12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2007.11.087
CHEMBL252610 94723 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 589 12 3 7 5.0 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)CC12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2007.11.087
9845853 128542 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 435 7 2 3 5.3 COc1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
CHEMBL366654 128542 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 435 7 2 3 5.3 COc1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
44593546 178862 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 531 6 2 6 4.9 CN1CC(C)(NC(=O)Nc2nc(C(C)(C)C)cs2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL468695 178862 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 531 6 2 6 4.9 CN1CC(C)(NC(=O)Nc2nc(C(C)(C)C)cs2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
44445853 154672 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 473 7 3 6 3.5 CC(=O)c1sc(NC(=O)N[C@@H]2CNC[C@@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL399134 154672 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 473 7 3 6 3.5 CC(=O)c1sc(NC(=O)N[C@@H]2CNC[C@@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
11144348 16591 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 424 6 2 3 5.7 N#Cc1cccc(NC(=O)Nc2cccc(CN3CCC(Cc4ccccc4)CC3)c2)c1 10.1021/jm0201767
CHEMBL123957 16591 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 424 6 2 3 5.7 N#Cc1cccc(NC(=O)Nc2cccc(CN3CCC(Cc4ccccc4)CC3)c2)c1 10.1021/jm0201767
11048445 16773 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 439 6 3 3 5.7 O=C(Nc1ccc2[nH]ncc2c1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL124390 16773 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 439 6 3 3 5.7 O=C(Nc1ccc2[nH]ncc2c1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
11091447 169493 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 439 6 3 3 5.7 O=C(Nc1ccc2c[nH]nc2c1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL442210 169493 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 439 6 3 3 5.7 O=C(Nc1ccc2c[nH]nc2c1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
6918497 113493 None 1 Mouse Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against I-Eotaxin alpha binding to mouse CCR3 receptorsInhibitory activity against I-Eotaxin alpha binding to mouse CCR3 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against I-Eotaxin alpha binding to mouse CCR3 receptorsInhibitory activity against I-Eotaxin alpha binding to mouse CCR3 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against I-Eotaxin alpha binding to mouse CCR3 receptorsInhibitory activity against I-Eotaxin alpha binding to mouse CCR3 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
10916572 18524 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 408 8 0 2 6.2 N#CC(CCCN1CCC(Cc2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL127395 18524 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 408 8 0 2 6.2 N#CC(CCCN1CCC(Cc2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11102400 118158 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 449 6 2 3 5.7 O=C(Nc1cc(F)ccc1F)Nc1ccccc1CN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm0201767
CHEMBL340656 118158 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 449 6 2 3 5.7 O=C(Nc1cc(F)ccc1F)Nc1ccccc1CN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm0201767
10906911 17996 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 477 8 3 4 5.4 COc1cccc(NC(=O)Nc2ccc(CO)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL126220 17996 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 477 8 3 4 5.4 COc1cccc(NC(=O)Nc2ccc(CO)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
68826395 103561 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 5.0 CC(=O)c1cccc(NC(=O)NCCCN2[C@H]3CC[C@@H]2C[C@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
CHEMBL3085118 103561 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 5.0 CC(=O)c1cccc(NC(=O)NCCCN2[C@H]3CC[C@@H]2C[C@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
10984360 97002 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 537 8 1 7 5.7 CCOC(=O)c1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 10.1016/s0960-894x(01)00176-7
CHEMBL266181 97002 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 537 8 1 7 5.7 CCOC(=O)c1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 10.1016/s0960-894x(01)00176-7
44295375 168256 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 419 6 2 4 3.5 CN(C)c1ccc(NC(=O)NCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL433086 168256 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 419 6 2 4 3.5 CN(C)c1ccc(NC(=O)NCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)cc1 10.1016/s0960-894x(02)00206-8
9840971 99793 None 42 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 342 7 1 5 2.5 CCOC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL284954 99793 None 42 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 342 7 1 5 2.5 CCOC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
11733139 16911 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 454 7 3 4 5.2 N#Cc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL125132 16911 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 454 7 3 4 5.2 N#Cc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
44289699 167918 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 409 6 2 3 3.9 CC(=O)c1cccc(NC(=O)NCCCN2C[C@@H]3Cc4ccc(F)cc4C[C@H]3C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43066 167918 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 409 6 2 3 3.9 CC(=O)c1cccc(NC(=O)NCCCN2C[C@@H]3Cc4ccc(F)cc4C[C@H]3C2)c1 10.1016/j.bmcl.2004.01.059
10474776 113721 None 32 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(03)00748-0
CHEMBL33227 113721 None 32 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(03)00748-0
44390842 123904 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL362490 123904 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
44295485 101927 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 497 12 3 4 5.4 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccc(F)cc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL300699 101927 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 497 12 3 4 5.4 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccc(F)cc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
22393287 168067 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL43173 168067 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
11316656 70286 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 441 6 2 2 5.6 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL194141 70286 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 441 6 2 2 5.6 O=C(Nc1ccc(F)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
10474776 113721 None 32 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
22393287 168067 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL43173 168067 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 451 8 2 6 3.5 Cn1nnnc1-c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.01.059
44593553 178472 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 489 6 2 6 3.9 Cc1csc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1016/j.bmcl.2008.11.002
CHEMBL465272 178472 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 489 6 2 6 3.9 Cc1csc(NC(=O)NC2(C)CN(C)C(=O)OC2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)n1 10.1016/j.bmcl.2008.11.002
44593546 178862 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 531 6 2 6 4.9 CN1CC(C)(NC(=O)Nc2nc(C(C)(C)C)cs2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
CHEMBL468695 178862 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 531 6 2 6 4.9 CN1CC(C)(NC(=O)Nc2nc(C(C)(C)C)cs2)C(CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O 10.1016/j.bmcl.2008.11.002
44390911 63828 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 515 8 2 6 4.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(Cl)cc3Cl)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180229 63828 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 515 8 2 6 4.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(Cl)cc3Cl)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44390859 131858 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccccc3F)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL369331 131858 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 465 8 2 6 3.7 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccccc3F)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44447369 94664 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H]([C@H](O)c1ccccc1)N(C)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL252222 94664 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H]([C@H](O)c1ccccc1)N(C)C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44419308 141617 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 509 10 2 4 5.4 CCC(=O)N1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
CHEMBL384649 141617 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 509 10 2 4 5.4 CCC(=O)N1CC[C@@H](Cc2ccc(F)cc2)C[C@@H]1CCCNC(=O)Nc1cc(C(C)=O)cc(C(C)=O)c1 10.1016/j.bmcl.2006.08.012
44455872 155605 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
CHEMBL404202 155605 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 receptor expressed in CHO cells
ChEMBL 467 9 2 4 5.1 CC(=O)c1cc(NC(=O)N[C@@H](C)CCN2CCC[C@@H](Cc3ccc(F)cc3)C2)cc(C(C)=O)c1 10.1016/j.bmcl.2007.11.067
44295622 101546 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 465 10 3 4 4.7 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@@H](O)C(C)C)c1 10.1016/s0960-894x(02)00206-8
CHEMBL297904 101546 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 465 10 3 4 4.7 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@@H](O)C(C)C)c1 10.1016/s0960-894x(02)00206-8
44295286 188406 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 431 8 2 3 4.0 C[S+]([O-])c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50034 188406 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 431 8 2 3 4.0 C[S+]([O-])c1cccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44295672 188864 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 439 6 1 3 5.0 COc1cccc(NC(=O)N2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50535 188864 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 439 6 1 3 5.0 COc1cccc(NC(=O)N2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44295641 189437 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 453 9 4 5 3.4 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2C(C)(O)O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51244 189437 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 453 9 4 5 3.4 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2C(C)(O)O)c1 10.1016/s0960-894x(02)00206-8
23509695 189848 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCOC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL51584 189848 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 441 6 1 4 4.0 COc1cccc(NC(=O)N2CCOC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
44295364 196650 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL54290 196650 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
22257689 16588 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 446 7 1 2 6.0 Cc1ccc(C(=O)NC(CN2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
CHEMBL123943 16588 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 446 7 1 2 6.0 Cc1ccc(C(=O)NC(CN2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
44346211 163988 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 537 10 2 5 6.5 COc1cc(NC(=O)NC(CC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(C)C)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
CHEMBL420709 163988 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 537 10 2 5 6.5 COc1cc(NC(=O)NC(CC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(C)C)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
44295130 101251 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 362 6 2 3 3.6 N#Cc1cccc(NC(=O)NCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL295726 101251 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 362 6 2 3 3.6 N#Cc1cccc(NC(=O)NCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
44295528 101962 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 336 4 0 2 4.0 Fc1ccc(CCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL300905 101962 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 336 4 0 2 4.0 Fc1ccc(CCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)cc1 10.1016/s0960-894x(02)00206-8
22393370 189964 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 390 7 2 3 4.3 Cc1ccc(CC2CCN(CCCNC(=O)Nc3cccc(C#N)c3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51676 189964 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 390 7 2 3 4.3 Cc1ccc(CC2CCN(CCCNC(=O)Nc3cccc(C#N)c3)CC2)cc1 10.1016/s0960-894x(02)00206-8
22393398 195962 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 390 8 2 3 4.4 N#Cc1cccc(NC(=O)NCCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL54143 195962 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 390 8 2 3 4.4 N#Cc1cccc(NC(=O)NCCCCN2CCC(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(02)00206-8
10979426 17970 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 298 7 3 2 2.7 O=C(NCCCO)NC(Cc1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL126106 17970 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 298 7 3 2 2.7 O=C(NCCCO)NC(Cc1ccccc1)c1ccccc1 10.1021/jm0201767
44295102 188057 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 405 7 1 4 3.4 COc1ccc(C(=O)NCCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL49702 188057 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 405 7 1 4 3.4 COc1ccc(C(=O)NCCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)cc1 10.1016/s0960-894x(02)00206-8
10985078 114802 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm0201767
CHEMBL333865 114802 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm0201767
11081509 18550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 492 6 2 3 6.9 N#Cc1cccc(NC(=O)Nc2c(CN3CCC(Cc4ccc(F)cc4)CC3)ccc3ccccc23)c1 10.1021/jm0201767
CHEMBL127534 18550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 492 6 2 3 6.9 N#Cc1cccc(NC(=O)Nc2c(CN3CCC(Cc4ccc(F)cc4)CC3)ccc3ccccc23)c1 10.1021/jm0201767
11004826 17995 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 447 7 3 3 5.4 O=C(Nc1ccccc1)Nc1cccc(CO)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL126218 17995 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 447 7 3 3 5.4 O=C(Nc1ccccc1)Nc1cccc(CO)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44295470 188936 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 425 5 1 3 4.8 COc1cccc(NC(=O)N2CCCC(N3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50645 188936 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 425 5 1 3 4.8 COc1cccc(NC(=O)N2CCCC(N3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1016/s0960-894x(02)00206-8
22022834 113400 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 472 7 1 2 6.4 Cc1ccc(C(=O)NC(CN2CC3CCC2CC3Cc2ccc(Cl)c(Cl)c2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
CHEMBL331672 113400 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 472 7 1 2 6.4 Cc1ccc(C(=O)NC(CN2CC3CCC2CC3Cc2ccc(Cl)c(Cl)c2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
11072275 16804 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 632 10 3 5 5.9 COC(=O)N1CCC(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0201767
CHEMBL124585 16804 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 632 10 3 5 5.9 COC(=O)N1CCC(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0201767
25024651 116100 None 0 Human Binding pIC50 = 6.3 6.3 39 3
Inhibition of CCR3 in human eosinophil assessed as inhibition of shape change by autofluorescence assayInhibition of CCR3 in human eosinophil assessed as inhibition of shape change by autofluorescence assay
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355956 116100 None 0 Human Binding pIC50 = 6.3 6.3 39 3
Inhibition of CCR3 in human eosinophil assessed as inhibition of shape change by autofluorescence assayInhibition of CCR3 in human eosinophil assessed as inhibition of shape change by autofluorescence assay
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
10257335 100499 None 2 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 565 6 2 4 3.5 CCOC(=O)[C@H](Cc1cc(I)c(O)c(I)c1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL290565 100499 None 2 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 565 6 2 4 3.5 CCOC(=O)[C@H](Cc1cc(I)c(O)c(I)c1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
11227406 94398 None 2 Mouse Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 mins
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
CHEMBL250689 94398 None 2 Mouse Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from BALB/c mouse CCR3 expressed in CHO cells after 30 mins
ChEMBL 465 7 2 3 5.7 CC(=O)c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2007.03.065
44390858 63924 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 423 6 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NCC2CCN(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL180534 63924 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 423 6 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NCC2CCN(Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.11.006
10928826 17807 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 472 7 3 4 5.3 N#Cc1cccc(NC(=O)Nc2ccc(CO)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL125884 17807 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 472 7 3 4 5.3 N#Cc1cccc(NC(=O)Nc2ccc(CO)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
9951882 179275 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 381 8 2 3 4.2 COc1cccc(NC(=O)NCCCN2CCCC(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL47220 179275 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 381 8 2 3 4.2 COc1cccc(NC(=O)NCCCN2CCCC(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2004.01.059
44295230 189226 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 379 5 1 3 3.2 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51038 189226 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 379 5 1 3 3.2 O=C(NCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
44290041 172831 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 409 6 2 3 3.9 CC(=O)c1cccc(NC(=O)NCCCN2C[C@H]3Cc4ccc(F)cc4C[C@H]3C2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL45064 172831 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 409 6 2 3 3.9 CC(=O)c1cccc(NC(=O)NCCCN2C[C@H]3Cc4ccc(F)cc4C[C@H]3C2)c1 10.1016/j.bmcl.2004.01.059
44281790 169316 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 420 6 1 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL440844 169316 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 420 6 1 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11082578 118134 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 603 10 3 3 7.5 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cc(F)ccc1F 10.1021/jm0201767
CHEMBL340491 118134 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 603 10 3 3 7.5 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cc(F)ccc1F 10.1021/jm0201767
44447366 94663 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(C)[C@H](C)[C@H](O)c1ccccc1 10.1016/j.bmcl.2007.11.087
CHEMBL252221 94663 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 453 9 4 8 1.8 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(C)[C@H](C)[C@H](O)c1ccccc1 10.1016/j.bmcl.2007.11.087
44447141 94640 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 523 11 3 7 3.4 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)CC(F)(F)F 10.1016/j.bmcl.2007.11.087
CHEMBL252034 94640 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 523 11 3 7 3.4 C[C@@H](NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](O)CN(CCCc1ccc(F)cc1)CC(F)(F)F 10.1016/j.bmcl.2007.11.087
9818195 110420 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 311 7 1 3 3.0 CCOC(=O)[C@H](CCc1ccccc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL32413 110420 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 311 7 1 3 3.0 CCOC(=O)[C@H](CCc1ccccc1)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
10995329 18188 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 563 13 4 4 5.5 O=C(NCCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL126978 18188 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 563 13 4 4 5.5 O=C(NCCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44419327 83249 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 393 8 3 3 4.4 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218581 83249 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 393 8 3 3 4.4 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
44447155 155013 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 511 11 3 7 2.9 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)C(C)=O)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL401002 155013 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 511 11 3 7 2.9 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)C(C)=O)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44445843 94294 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 587 7 2 7 5.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)OC(C)(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL250054 94294 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 587 7 2 7 5.5 CC(=O)c1sc(NC(=O)N[C@@H]2CCN(C(=O)OC(C)(C)C)C[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390978 64593 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NCC2CCCN(CCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
CHEMBL181575 64593 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 437 7 2 6 3.1 Cn1nnnc1-c1cccc(NC(=O)NCC2CCCN(CCc3ccc(F)cc3)C2)c1 10.1016/j.bmcl.2004.11.006
3492 692 None 0 Human Binding pIC50 = 8.2 8.2 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
9868459 692 None 0 Human Binding pIC50 = 8.2 8.2 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
CHEMBL50593 692 None 0 Human Binding pIC50 = 8.2 8.2 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
11179592 69614 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 501 6 2 2 6.2 O=C(Nc1ccc(Br)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
CHEMBL193442 69614 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 501 6 2 2 6.2 O=C(Nc1ccc(Br)cc1)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 10.1021/jm049530m
44440431 146550 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 607 9 0 7 5.2 Cc1c(CN(CCc2ccc([N+](=O)[O-])cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL392217 146550 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 607 9 0 7 5.2 Cc1c(CN(CCc2ccc([N+](=O)[O-])cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(F)cc2)n1C 10.1016/j.bmcl.2007.05.035
44445890 155039 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 9 2 7 4.1 CC(=O)CN1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
CHEMBL401115 155039 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 543 9 2 7 4.1 CC(=O)CN1CC[C@@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)[C@H](NC(=O)Nc2nc(C)c(C(C)=O)s2)C1 10.1016/j.bmcl.2007.03.065
11226588 94818 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 547 10 2 6 5.2 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN(CCCc2ccc(F)cc2)CC(F)(F)F)c1 10.1016/j.bmcl.2007.11.087
CHEMBL253211 94818 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 547 10 2 6 5.2 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN(CCCc2ccc(F)cc2)CC(F)(F)F)c1 10.1016/j.bmcl.2007.11.087
44295201 171445 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 11 3 4 5.1 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@H](O)CC(C)C)c1 10.1016/s0960-894x(02)00206-8
CHEMBL446144 171445 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 11 3 4 5.1 CC(=O)c1cccc(NC(=O)NCCCN2CC[C@H](Cc3ccccc3)C[C@@H]2[C@H](O)CC(C)C)c1 10.1016/s0960-894x(02)00206-8
44295328 194859 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 7 2 2 5.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL53673 194859 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 7 2 2 5.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(02)00206-8
11026367 16489 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 429 7 2 3 5.8 COc1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL123511 16489 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 429 7 2 3 5.8 COc1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
11060510 16509 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 533 10 3 3 6.1 CC(C)NC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL123622 16509 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 533 10 3 3 6.1 CC(C)NC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11004681 16839 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 439 6 3 3 5.7 O=C(Nc1cccc(CN2CCC(Cc3ccccc3)CC2)c1)Nc1ccc2[nH]ncc2c1 10.1021/jm0201767
CHEMBL124748 16839 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 439 6 3 3 5.7 O=C(Nc1cccc(CN2CCC(Cc3ccccc3)CC2)c1)Nc1ccc2[nH]ncc2c1 10.1021/jm0201767
7072714 110519 None 1 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 490 11 3 6 3.5 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL32468 110519 None 1 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 490 11 3 6 3.5 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1 10.1016/s0960-894x(01)00248-7
44440413 93641 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 612 8 0 5 6.4 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246549 93641 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 612 8 0 5 6.4 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2007.05.035
10983980 18053 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 505 8 2 5 5.7 COC(=O)c1ccc(NC(=O)Nc2cccc(OC)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL126520 18053 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 505 8 2 5 5.7 COC(=O)c1ccc(NC(=O)Nc2cccc(OC)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44295463 162098 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 429 7 1 4 3.1 O=S(=O)(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL415950 162098 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 429 7 1 4 3.1 O=S(=O)(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
44419314 83333 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
CHEMBL218997 83333 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 376 7 3 3 4.1 N#Cc1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccccc3)CCN2)c1 10.1016/j.bmcl.2006.08.012
44346154 168764 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 489 7 2 4 4.7 C[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
CHEMBL436363 168764 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 489 7 2 4 4.7 C[C@H](CN1C2CCC1CC(Cc1ccc(Cl)cc1)C2)NC(=O)Nc1cccc(S(C)(=O)=O)c1 10.1016/s0960-894x(03)00748-0
11511522 67889 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 491 8 0 6 3.1 COc1ccc(OC)c(S(=O)(=O)N2CCC(CN3CCN(Cc4ccc(F)cc4)CC3)CC2)c1 10.1016/j.bmcl.2011.09.013
CHEMBL1910163 67889 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 491 8 0 6 3.1 COc1ccc(OC)c(S(=O)(=O)N2CCC(CN3CCN(Cc4ccc(F)cc4)CC3)CC2)c1 10.1016/j.bmcl.2011.09.013
44295407 189750 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 433 6 1 3 4.3 O=C(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)C12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(02)00206-8
CHEMBL51507 189750 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 433 6 1 3 4.3 O=C(NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)C12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(02)00206-8
9845853 128542 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 435 7 2 3 5.3 COc1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
CHEMBL366654 128542 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 435 7 2 3 5.3 COc1cccc(NC(=O)NC2CCCCC2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
10929194 17981 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 500 7 2 5 5.6 COC(=O)c1ccc(NC(=O)Nc2cccc(C#N)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL126163 17981 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 500 7 2 5 5.6 COC(=O)c1ccc(NC(=O)Nc2cccc(C#N)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
44295065 184397 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 405 7 1 4 3.4 COc1ccccc1C(=O)NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3 10.1016/s0960-894x(02)00206-8
CHEMBL48401 184397 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 405 7 1 4 3.4 COc1ccccc1C(=O)NCCCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3 10.1016/s0960-894x(02)00206-8
10474776 113721 None 32 Human Binding pIC50 = 8.2 8.2 - 0
Agonistic activity against C-C chemokine receptor type 3 by displacing [125I]-MCP-4 radioligand, using CCR3 binding assayAgonistic activity against C-C chemokine receptor type 3 by displacing [125I]-MCP-4 radioligand, using CCR3 binding assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL33227 113721 None 32 Human Binding pIC50 = 8.2 8.2 - 0
Agonistic activity against C-C chemokine receptor type 3 by displacing [125I]-MCP-4 radioligand, using CCR3 binding assayAgonistic activity against C-C chemokine receptor type 3 by displacing [125I]-MCP-4 radioligand, using CCR3 binding assay
ChEMBL 378 6 1 5 3.3 COC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
22966050 84170 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 455 10 3 4 4.2 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCO)c1 10.1016/j.bmcl.2006.08.012
CHEMBL220801 84170 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to CCR3Binding affinity to CCR3
ChEMBL 455 10 3 4 4.2 CC(=O)c1cccc(NC(=O)NCCC[C@H]2C[C@H](Cc3ccc(F)cc3)CCN2CCO)c1 10.1016/j.bmcl.2006.08.012
44295282 101712 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 414 8 2 4 4.2 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(02)00206-8
CHEMBL299170 101712 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 414 8 2 4 4.2 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(02)00206-8
44295591 188323 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 465 11 3 4 4.9 CCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL49921 188323 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 465 11 3 4 4.9 CCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
44593555 188892 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR3 at 10 uMInhibition of CCR3 at 10 uM
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188892 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR3 at 10 uMInhibition of CCR3 at 10 uM
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
10874762 16811 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 500 7 2 5 5.6 COC(=O)c1cccc(NC(=O)Nc2cccc(C#N)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL124628 16811 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 500 7 2 5 5.6 COC(=O)c1cccc(NC(=O)Nc2cccc(C#N)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44290020 179132 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 435 8 2 4 4.5 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cccc(-n2ccnc2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL47122 179132 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 435 8 2 4 4.5 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cccc(-n2ccnc2)c1 10.1016/j.bmcl.2004.01.059
68826395 103561 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 5.0 CC(=O)c1cccc(NC(=O)NCCCN2[C@H]3CC[C@@H]2C[C@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
CHEMBL3085118 103561 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 5.0 CC(=O)c1cccc(NC(=O)NCCCN2[C@H]3CC[C@@H]2C[C@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
44445850 94135 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 473 7 3 6 3.5 CC(=O)c1sc(NC(=O)N[C@@H]2CNC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL249056 94135 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 473 7 3 6 3.5 CC(=O)c1sc(NC(=O)N[C@@H]2CNC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390898 64586 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 9 2 6 4.2 CCc1cc(NC(=O)N[C@@H]2CCCN(CCCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL181528 64586 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 479 9 2 6 4.2 CCc1cc(NC(=O)N[C@@H]2CCCN(CCCCc3ccc(F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44290029 179253 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 436 8 2 4 4.9 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cccc(-c2cnco2)c1 10.1016/j.bmcl.2004.01.059
CHEMBL47211 179253 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 436 8 2 4 4.9 O=C(NCCCN1CCC[C@@H](Cc2ccc(F)cc2)C1)Nc1cccc(-c2cnco2)c1 10.1016/j.bmcl.2004.01.059
22393474 96603 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 7 2 2 5.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(C(F)(F)F)c1 10.1016/s0960-894x(02)00206-8
CHEMBL262918 96603 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 437 7 2 2 5.3 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc(C(F)(F)F)c1 10.1016/s0960-894x(02)00206-8
44295288 189457 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 447 8 2 4 3.7 CS(=O)(=O)c1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL51259 189457 None 0 Human Binding pIC50 = 7.2 7.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 447 8 2 4 3.7 CS(=O)(=O)c1ccc(NC(=O)NCCCN2CCC(Cc3ccc(F)cc3)CC2)cc1 10.1016/s0960-894x(02)00206-8
44295510 101901 None 0 Human Binding pIC50 = 6.2 6.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 401 5 2 4 3.3 N#Cc1cccc(NC(=O)NCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)c1 10.1016/s0960-894x(02)00206-8
CHEMBL300472 101901 None 0 Human Binding pIC50 = 6.2 6.2 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 401 5 2 4 3.3 N#Cc1cccc(NC(=O)NCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)c1 10.1016/s0960-894x(02)00206-8
10591473 64908 None 7 Human Binding pIC50 = 5.2 5.2 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 279 5 0 1 4.2 c1ccc(CCN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
CHEMBL18222 64908 None 7 Human Binding pIC50 = 5.2 5.2 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 279 5 0 1 4.2 c1ccc(CCN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
11812728 16758 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 471 7 2 5 4.8 O=C(NCc1ccc2c(c1)OCO2)Nc1ccccc1CN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm0201767
CHEMBL124336 16758 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 471 7 2 5 4.8 O=C(NCc1ccc2c(c1)OCO2)Nc1ccccc1CN1CCC(C(=O)c2ccccc2)CC1 10.1021/jm0201767
10000888 76004 None 1 Human Binding pIC50 = 6.1 6.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 397 6 1 5 4.2 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL20539 76004 None 1 Human Binding pIC50 = 6.1 6.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 397 6 1 5 4.2 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(01)00176-7
10142792 93794 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93794 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cellsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11069916 16565 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 424 6 2 3 5.7 N#Cc1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL123791 16565 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 424 6 2 3 5.7 N#Cc1cccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
10993686 117001 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 429 7 2 3 5.8 COc1ccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
CHEMBL338543 117001 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 429 7 2 3 5.8 COc1ccc(NC(=O)Nc2ccccc2CN2CCC(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
57394442 67891 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 407 8 2 3 4.2 O=C(NCCCCN1CCC(Oc2ccc(F)cc2)C1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2011.09.013
CHEMBL1910165 67891 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 407 8 2 3 4.2 O=C(NCCCCN1CCC(Oc2ccc(F)cc2)C1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2011.09.013
11072063 16612 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 597 11 3 4 7.2 COc1ccc(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm0201767
CHEMBL124084 16612 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 597 11 3 4 7.2 COc1ccc(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm0201767
11026461 16947 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 434 8 2 3 4.7 O=C(NCCN1CCCCC1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL125325 16947 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 434 8 2 3 4.7 O=C(NCCN1CCCCC1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
11005432 168461 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 487 8 2 5 5.6 COC(=O)c1ccc(CN2CCC(Cc3ccccc3)CC2)c(NC(=O)Nc2cccc(OC)c2)c1 10.1021/jm0201767
CHEMBL434437 168461 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 487 8 2 5 5.6 COC(=O)c1ccc(CN2CCC(Cc3ccccc3)CC2)c(NC(=O)Nc2cccc(OC)c2)c1 10.1021/jm0201767
11385474 78567 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)NC2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1021/jm049530m
CHEMBL2112050 78567 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 453 7 2 3 5.5 COc1cccc(NC(=O)NC2CCCC(CN3CCC(Cc4ccc(F)cc4)CC3)C2)c1 10.1021/jm049530m
44346023 15101 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(=O)NC(CC2CCN(Cc3ccc(C)c(C)c3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
CHEMBL120957 15101 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(=O)NC(CC2CCN(Cc3ccc(C)c(C)c3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
10873705 99390 None 7 Human Binding pIC50 = 7.1 7.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.8 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL282285 99390 None 7 Human Binding pIC50 = 7.1 7.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.8 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00176-7
44440421 93583 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 593 8 1 6 5.3 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(N)cc2)n1C 10.1016/j.bmcl.2007.05.035
CHEMBL246339 93583 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]eotaxin from CCR3 receptor in human eosinophilsDisplacement of [125I]eotaxin from CCR3 receptor in human eosinophils
ChEMBL 593 8 1 6 5.3 Cc1c(CN(CCc2ccc(Cl)cc2)C2CCN(C(=O)c3c(F)cccc3F)CC2)c(=O)n(-c2ccc(N)cc2)n1C 10.1016/j.bmcl.2007.05.035
3492 692 None 0 Human Binding pIC50 = 8.1 8.1 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
9868459 692 None 0 Human Binding pIC50 = 8.1 8.1 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
CHEMBL50593 692 None 0 Human Binding pIC50 = 8.1 8.1 - 1
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 10.1016/s0960-894x(02)00206-8
9800669 109555 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 392 7 1 5 3.7 CCOC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL32210 109555 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 392 7 1 5 3.7 CCOC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
11070954 16786 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 485 7 3 4 4.9 N#Cc1cccc(NC(=O)Nc2ccc(C(N)=O)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL124473 16786 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 485 7 3 4 4.9 N#Cc1cccc(NC(=O)Nc2ccc(C(N)=O)cc2CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
10962347 18504 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 516 8 3 4 5.5 CNC(=O)c1ccc(NC(=O)Nc2cccc(C(C)=O)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
CHEMBL127281 18504 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 516 8 3 4 5.5 CNC(=O)c1ccc(NC(=O)Nc2cccc(C(C)=O)c2)c(CN2CCC(Cc3ccc(F)cc3)CC2)c1 10.1021/jm0201767
11763035 169421 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 517 8 2 5 5.9 COC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL441656 169421 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 517 8 2 5 5.9 COC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
11753159 547 None 6 Human Binding pIC50 = 8.1 8.1 1 2
Antagonist activity at CCR3 assessed as inhibition of eotaxin bindingAntagonist activity at CCR3 assessed as inhibition of eotaxin binding
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
7679 547 None 6 Human Binding pIC50 = 8.1 8.1 1 2
Antagonist activity at CCR3 assessed as inhibition of eotaxin bindingAntagonist activity at CCR3 assessed as inhibition of eotaxin binding
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
CHEMBL2158814 547 None 6 Human Binding pIC50 = 8.1 8.1 1 2
Antagonist activity at CCR3 assessed as inhibition of eotaxin bindingAntagonist activity at CCR3 assessed as inhibition of eotaxin binding
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
44346210 168058 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 531 10 3 6 4.7 COc1cc(NC(=O)N[C@@H](CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)[C@H](C)O)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
CHEMBL431670 168058 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 531 10 3 6 4.7 COc1cc(NC(=O)N[C@@H](CN2C3CCC2CC(Cc2ccc(Cl)cc2)C3)[C@H](C)O)cc(OC)c1OC 10.1016/s0960-894x(03)00748-0
44295536 188542 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 12 3 4 5.3 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50233 188542 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 479 12 3 4 5.3 CCCC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 10.1016/s0960-894x(02)00206-8
9885355 100460 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 363 6 2 4 3.5 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
CHEMBL290119 100460 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 363 6 2 4 3.5 CCOC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)c1cccc2ccccc12 10.1016/s0960-894x(01)00248-7
44295353 188792 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 350 8 1 2 4.2 O=C(NCCCCN1CCC(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(02)00206-8
CHEMBL50401 188792 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 350 8 1 2 4.2 O=C(NCCCCN1CCC(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(02)00206-8
71454583 79726 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 4.9 CC(=O)c1cccc(NC(=O)NCCCN2CC3CCC2[C@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
CHEMBL2115412 79726 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.Inhibitory concentration against C-C chemokine receptor type 3 using human [125I]eotaxin.
ChEMBL 437 8 2 3 4.9 CC(=O)c1cccc(NC(=O)NCCCN2CC3CCC2[C@H](Cc2ccc(F)cc2)C3)c1 10.1016/j.bmcl.2004.01.059
11015975 16503 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 459 8 3 4 5.3 COc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
CHEMBL123585 16503 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 459 8 3 4 5.3 COc1cccc(NC(=O)Nc2ccccc2C(O)CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm0201767
44295118 189151 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 405 7 1 4 3.4 COc1cccc(C(=O)NCCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)c1 10.1016/s0960-894x(02)00206-8
CHEMBL50937 189151 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 405 7 1 4 3.4 COc1cccc(C(=O)NCCCCN2CC[C@@H]3[C@H](C2)c2cccc4c2N3CC4)c1 10.1016/s0960-894x(02)00206-8
57398008 67890 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 393 9 2 3 4.5 COc1ccc(Cl)cc1NC(=O)NCCCCN(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2011.09.013
CHEMBL1910164 67890 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assayDisplacement of [125I]-eotaxin from CCR3 expressed in RBL-2H3 cells by scintillation proximity assay
ChEMBL 393 9 2 3 4.5 COc1ccc(Cl)cc1NC(=O)NCCCCN(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2011.09.013
44390893 64395 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 515 8 2 6 4.5 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(C(F)(F)F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL181302 64395 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 515 8 2 6 4.5 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(C(F)(F)F)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
132072454 179830 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Antagonist activity at human CCR3 expressed in CHO-K1 cells by PathHunter beta-arrestin assayAntagonist activity at human CCR3 expressed in CHO-K1 cells by PathHunter beta-arrestin assay
ChEMBL 558 6 2 8 4.7 COC(=O)[C@H]1[C@@H](O)CC[C@H]2CN(C#N)[C@H](c3[nH]c4ccccc4c3CCn3cc(-c4cccc(Cl)c4)nn3)C[C@@H]21 10.1016/j.bmc.2020.115546
CHEMBL4744046 179830 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Antagonist activity at human CCR3 expressed in CHO-K1 cells by PathHunter beta-arrestin assayAntagonist activity at human CCR3 expressed in CHO-K1 cells by PathHunter beta-arrestin assay
ChEMBL 558 6 2 8 4.7 COC(=O)[C@H]1[C@@H](O)CC[C@H]2CN(C#N)[C@H](c3[nH]c4ccccc4c3CCn3cc(-c4cccc(Cl)c4)nn3)C[C@@H]21 10.1016/j.bmc.2020.115546
44295558 102018 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 365 4 1 3 2.8 O=C(NCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
CHEMBL301332 102018 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 365 4 1 3 2.8 O=C(NCCN1CC[C@@H]2[C@H](C1)c1cccc3c1N2CC3)c1ccc(F)cc1 10.1016/s0960-894x(02)00206-8
10934382 16783 None 26 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 265 4 0 1 4.1 c1ccc(CC2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
CHEMBL124457 16783 None 26 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 265 4 0 1 4.1 c1ccc(CC2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
11828013 17414 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 581 11 3 3 6.9 O=C(NCc1ccccc1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL125753 17414 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 581 11 3 3 6.9 O=C(NCc1ccccc1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11049424 117170 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 505 9 3 3 5.3 CNC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL339349 117170 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 505 9 3 3 5.3 CNC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
9972570 69853 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 308 7 0 2 3.8 c1ccc(CCCCN2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
CHEMBL19375 69853 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 308 7 0 2 3.8 c1ccc(CCCCN2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm0201767
10458117 16593 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 486 6 2 5 5.5 N#Cc1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
CHEMBL123961 16593 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 486 6 2 5 5.5 N#Cc1cccc(NC(=O)Nc2cc3c(cc2CN2CCC(Cc4ccc(F)cc4)CC2)OCO3)c1 10.1021/jm0201767
44346178 114320 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 423 8 1 4 5.0 Cc1ccc(C(=O)NC(CC2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
CHEMBL333040 114320 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligandBinding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand
ChEMBL 423 8 1 4 5.0 Cc1ccc(C(=O)NC(CC2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)C(C)C)cc1 10.1016/s0960-894x(03)00748-0
44447377 94884 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 499 11 4 8 2.2 CCN(C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](C)[C@H](O)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
CHEMBL253666 94884 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 499 11 4 8 2.2 CCN(C[C@H](O)[C@@H](C)NC(=O)Nc1cccc(-c2nnnn2C)c1)[C@@H](C)[C@H](O)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.087
44295327 188490 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 414 8 2 4 4.2 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccccc1[N+](=O)[O-] 10.1016/s0960-894x(02)00206-8
CHEMBL50158 188490 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 414 8 2 4 4.2 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccccc1[N+](=O)[O-] 10.1016/s0960-894x(02)00206-8
44447150 94998 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 551 12 3 7 3.9 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC(F)(F)F)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
CHEMBL254471 94998 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cellsDisplacement of [125I] eotaxin from human CCR3 receptor in CHO cells
ChEMBL 551 12 3 7 3.9 CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC(F)(F)F)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2007.11.087
44295326 169179 None 0 Human Binding pIC50 = 8.1 8.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 414 8 2 4 4.2 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc([N+](=O)[O-])c1 10.1016/s0960-894x(02)00206-8
CHEMBL439744 169179 None 0 Human Binding pIC50 = 8.1 8.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 414 8 2 4 4.2 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1cccc([N+](=O)[O-])c1 10.1016/s0960-894x(02)00206-8
44387850 60534 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 430 6 2 3 5.2 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
CHEMBL175679 60534 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 430 6 2 3 5.2 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC(Cc3ccccc3)CC2)c1 10.1021/jm049530m
11236236 77989 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 448 6 2 3 5.3 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL2096696 77989 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 448 6 2 3 5.3 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11224689 78000 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 448 6 2 3 5.3 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL2096764 78000 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cellsInhibition of [125I]eotaxin binding to human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 448 6 2 3 5.3 N#Cc1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
10939698 161764 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 475 7 2 4 5.7 COC(=O)c1cccc(NC(=O)Nc2ccccc2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
CHEMBL413113 161764 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 475 7 2 4 5.7 COC(=O)c1cccc(NC(=O)Nc2ccccc2)c1CN1CCC(Cc2ccc(F)cc2)CC1 10.1021/jm0201767
44570582 178522 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 477 10 2 6 3.9 CCCN(CCCc1ccc(F)cc1)C[C@@H]1OC(=O)N(C)C[C@H]1NC(=O)Nc1nc(C)cs1 10.1016/j.bmcl.2008.11.002
CHEMBL465943 178522 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to CCR3 receptorBinding affinity to CCR3 receptor
ChEMBL 477 10 2 6 3.9 CCCN(CCCc1ccc(F)cc1)C[C@@H]1OC(=O)N(C)C[C@H]1NC(=O)Nc1nc(C)cs1 10.1016/j.bmcl.2008.11.002
44445846 94476 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 587 7 2 7 5.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)OC(C)(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
CHEMBL251078 94476 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 minsDisplacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
ChEMBL 587 7 2 7 5.5 CC(=O)c1sc(NC(=O)N[C@@H]2CN(C(=O)OC(C)(C)C)CC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1016/j.bmcl.2007.03.065
44390882 122867 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 461 8 2 6 3.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(C)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
CHEMBL360529 122867 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Evaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cellsEvaluated for inhibition of human C-C chemokine receptor type 3 expressed in CHO cells
ChEMBL 461 8 2 6 3.8 CCc1cc(NC(=O)NC[C@@H]2CCCN(CCc3ccc(C)cc3)C2)cc(-c2nnnn2C)c1 10.1016/j.bmcl.2004.11.006
44295543 102041 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 427 7 2 2 4.7 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NC12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(02)00206-8
CHEMBL301503 102041 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxinIn vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin
ChEMBL 427 7 2 2 4.7 O=C(NCCCN1CCC(Cc2ccc(F)cc2)CC1)NC12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(02)00206-8
11811443 16624 None 2 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 399 6 2 2 5.8 O=C(Nc1ccccc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL124134 16624 None 2 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 399 6 2 2 5.8 O=C(Nc1ccccc1)Nc1ccccc1CN1CCC(Cc2ccccc2)CC1 10.1021/jm0201767
6995527 111962 None 2 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 221 4 1 3 1.4 CCOC(=O)[C@H](C)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
CHEMBL32878 111962 None 2 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligandInhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand
ChEMBL 221 4 1 3 1.4 CCOC(=O)[C@H](C)NC(=O)c1ccccc1 10.1016/s0960-894x(01)00248-7
9889700 118652 None 11 Human Binding pIC50 = 5.1 5.1 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL34166 118652 None 11 Human Binding pIC50 = 5.1 5.1 - 1
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11762084 16923 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 446 8 2 3 4.5 O=C(NCCc1ccc(F)cc1)Nc1ccccc1CN1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL125220 16923 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 446 8 2 3 4.5 O=C(NCCc1ccc(F)cc1)Nc1ccccc1CN1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
11060814 17180 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 567 10 3 3 7.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccccc1 10.1021/jm0201767
CHEMBL125618 17180 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cellsInhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
ChEMBL 567 10 3 3 7.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccccc1 10.1021/jm0201767
66615627 81309 None 0 Human Binding pKi = 9.7 9.7 158 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 536 8 1 4 6.1 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158790 81309 None 0 Human Binding pKi = 9.7 9.7 158 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 536 8 1 4 6.1 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
59296081 84117 None 0 Human Binding pKi = 9.5 9.5 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 608 9 3 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)N3CCC3)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207654 84117 None 0 Human Binding pKi = 9.5 9.5 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 608 9 3 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)N3CCC3)ccc12 10.1016/j.bmcl.2012.09.112
66615619 81302 None 0 Human Binding pKi = 9.3 9.3 79 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 522 8 1 4 5.7 Cc1c(Cl)ccc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158783 81302 None 0 Human Binding pKi = 9.3 9.3 79 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 522 8 1 4 5.7 Cc1c(Cl)ccc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.103
12001832 81303 None 0 Human Binding pKi = 9.3 9.3 63 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 522 8 1 4 5.7 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158784 81303 None 0 Human Binding pKi = 9.3 9.3 63 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 522 8 1 4 5.7 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
16040671 81310 None 0 Human Binding pKi = 9.2 9.2 56 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 502 8 1 4 5.4 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158791 81310 None 0 Human Binding pKi = 9.2 9.2 56 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 502 8 1 4 5.4 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
17963201 82298 None 0 Human Binding pKi = 9.2 9.2 31 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 539 5 1 5 5.0 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(C)c4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171047 82298 None 0 Human Binding pKi = 9.2 9.2 31 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 539 5 1 5 5.0 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(C)c4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
66615702 81306 None 0 Human Binding pKi = 9.1 9.1 100 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 522 8 1 4 5.8 C[C@](Cc1ccc(F)cc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158787 81306 None 0 Human Binding pKi = 9.1 9.1 100 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 522 8 1 4 5.8 C[C@](Cc1ccc(F)cc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59296033 84052 None 0 Human Binding pKi = 9.1 9.1 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 596 9 3 7 2.7 CN(C)S(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207286 84052 None 0 Human Binding pKi = 9.1 9.1 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 596 9 3 7 2.7 CN(C)S(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
59295968 84120 None 0 Human Binding pKi = 9.1 9.1 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3c(F)cccc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207657 84120 None 0 Human Binding pKi = 9.1 9.1 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3c(F)cccc23)CC1 10.1016/j.bmcl.2012.09.112
59296099 84124 None 0 Human Binding pKi = 9.1 9.1 50 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 494 7 3 5 3.7 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]nc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207660 84124 None 0 Human Binding pKi = 9.1 9.1 50 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 494 7 3 5 3.7 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]nc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
46931923 129342 None 0 Human Binding pKi = 9.1 9.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 6 1 5 4.2 Cc1cc(C(=O)N2CCCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670798 129342 None 0 Human Binding pKi = 9.1 9.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 6 1 5 4.2 Cc1cc(C(=O)N2CCCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
59295928 84049 None 0 Human Binding pKi = 9 9.0 63 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccc(S(C)(=O)=O)cc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207283 84049 None 0 Human Binding pKi = 9 9.0 63 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccc(S(C)(=O)=O)cc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
66615606 81304 None 0 Human Binding pKi = 8.9 8.9 398 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 513 8 1 5 4.9 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(C#N)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158785 81304 None 0 Human Binding pKi = 8.9 8.9 398 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 513 8 1 5 4.9 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(C#N)c1Cl 10.1016/j.bmcl.2012.08.103
71462100 81311 None 0 Human Binding pKi = 8.9 8.9 39 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 502 8 1 4 5.4 Cc1cc(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158792 81311 None 0 Human Binding pKi = 8.9 8.9 39 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 502 8 1 4 5.4 Cc1cc(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
59295938 84128 None 0 Human Binding pKi = 8.9 8.9 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 521 7 3 5 3.6 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)cc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207664 84128 None 0 Human Binding pKi = 8.9 8.9 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 521 7 3 5 3.6 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)cc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
66615691 81308 None 0 Human Binding pKi = 8.8 8.8 125 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 518 8 1 4 5.9 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158789 81308 None 0 Human Binding pKi = 8.8 8.8 125 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 518 8 1 4 5.9 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
9870185 84130 None 0 Human Binding pKi = 8.8 8.8 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2207666 84130 None 0 Human Binding pKi = 8.8 8.8 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
59295931 84246 None 0 Human Binding pKi = 8.8 8.8 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 462 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208429 84246 None 0 Human Binding pKi = 8.8 8.8 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 462 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
59296010 84248 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 490 7 3 6 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208431 84248 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 490 7 3 6 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
71459762 84125 None 0 Human Binding pKi = 8.8 8.8 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 452 8 3 5 3.2 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C1CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207661 84125 None 0 Human Binding pKi = 8.8 8.8 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 452 8 3 5 3.2 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C1CC1 10.1016/j.bmcl.2012.09.112
9870185 84130 None 0 Human Binding pKi = 8.8 8.8 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207666 84130 None 0 Human Binding pKi = 8.8 8.8 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.112
56967066 129367 None 0 Human Binding pKi = 8.8 8.8 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 7 1 5 4.0 CCN(C)C(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670824 129367 None 0 Human Binding pKi = 8.8 8.8 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 7 1 5 4.0 CCN(C)C(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
66615617 81307 None 0 Human Binding pKi = 8.7 8.7 31 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158788 81307 None 0 Human Binding pKi = 8.7 8.7 31 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
71456722 81312 None 0 Human Binding pKi = 8.7 8.7 39 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 486 8 1 4 4.9 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158793 81312 None 0 Human Binding pKi = 8.7 8.7 39 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 486 8 1 4 4.9 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
69262172 81324 None 0 Human Binding pKi = 8.7 8.7 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158822 81324 None 0 Human Binding pKi = 8.7 8.7 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59295935 84044 None 0 Human Binding pKi = 8.7 8.7 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(F)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207278 84044 None 0 Human Binding pKi = 8.7 8.7 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(F)ccc12 10.1016/j.bmcl.2012.09.112
59295978 84119 None 0 Human Binding pKi = 8.7 8.7 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2c(F)cccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207656 84119 None 0 Human Binding pKi = 8.7 8.7 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2c(F)cccc12 10.1016/j.bmcl.2012.09.112
59296066 84127 None 0 Human Binding pKi = 8.7 8.7 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 487 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)cc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207663 84127 None 0 Human Binding pKi = 8.7 8.7 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 487 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)cc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
69347575 81323 None 0 Human Binding pKi = 8 8.0 10 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)[C@@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158821 81323 None 0 Human Binding pKi = 8 8.0 10 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)[C@@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072040 81338 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 490 8 1 4 5.2 O=C(O)[C@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158835 81338 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 490 8 1 4 5.2 O=C(O)[C@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072044 81340 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccccc1Cl)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158837 81340 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccccc1Cl)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072050 81342 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccccc1F)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158839 81342 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccccc1F)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072118 81344 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158841 81344 None 0 Human Binding pKi = 8 8.0 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
22397445 82271 None 0 Human Binding pKi = 8 8.0 2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 499 4 1 4 5.0 O=C(c1c[nH]c(=O)c2ccccc12)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171020 82271 None 0 Human Binding pKi = 8 8.0 2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 499 4 1 4 5.0 O=C(c1c[nH]c(=O)c2ccccc12)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
57718837 116076 None 0 Mouse Binding pKi = 8 8.0 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 414 7 1 2 6.4 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355932 116076 None 0 Mouse Binding pKi = 8 8.0 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 414 7 1 2 6.4 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
59295946 84047 None 0 Human Binding pKi = 8 8.0 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 612 11 5 8 1.7 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NCCO)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207281 84047 None 0 Human Binding pKi = 8 8.0 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 612 11 5 8 1.7 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NCCO)ccc12 10.1016/j.bmcl.2012.09.112
56965995 129340 None 0 Human Binding pKi = 8.0 8.0 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 497 6 2 5 3.3 CNC(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670796 129340 None 0 Human Binding pKi = 8.0 8.0 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 497 6 2 5 3.3 CNC(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
69260946 81325 None 0 Human Binding pKi = 7 7.0 -19 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.5 O=C(O)c1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158823 81325 None 0 Human Binding pKi = 7 7.0 -19 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.5 O=C(O)c1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71462103 81333 None 0 Human Binding pKi = 7 7.0 -2 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158830 81333 None 0 Human Binding pKi = 7 7.0 -2 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
17963227 82263 None 0 Human Binding pKi = 7 7.0 -39 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 539 5 0 5 5.1 Cc1ccc(S(=O)(=O)N(C)C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171013 82263 None 0 Human Binding pKi = 7 7.0 -39 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 539 5 0 5 5.1 Cc1ccc(S(=O)(=O)N(C)C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
9910169 82268 None 0 Human Binding pKi = 7 7.0 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 422 7 1 4 4.3 COc1cccc(C(=O)NCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171018 82268 None 0 Human Binding pKi = 7 7.0 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 422 7 1 4 4.3 COc1cccc(C(=O)NCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.08.124
17963336 82295 None 0 Human Binding pKi = 7 7.0 -5 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 536 5 1 6 4.3 N#Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171044 82295 None 0 Human Binding pKi = 7 7.0 -5 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 536 5 1 6 4.3 N#Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
118721192 116085 None 0 Rat Binding pKi = 7 7.0 4 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 458 8 1 4 6.0 CCOC(=O)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355941 116085 None 0 Rat Binding pKi = 7 7.0 4 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 458 8 1 4 6.0 CCOC(=O)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
10300214 84233 None 0 Human Binding pKi = 7 7.0 -6 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 492 9 2 5 5.0 O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208416 84233 None 0 Human Binding pKi = 7 7.0 -6 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 492 9 2 5 5.0 O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1 10.1016/j.bmcl.2012.09.113
44389685 64754 None 0 Human Binding pKi = 7 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 459 4 1 2 6.3 Cc1ccccc1NC(=O)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL181894 64754 None 0 Human Binding pKi = 7 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 459 4 1 2 6.3 Cc1ccccc1NC(=O)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
17989653 81493 None 0 Human Binding pKi = 7 7.0 - 1
Inhibition of CCR3 receptorInhibition of CCR3 receptor
ChEMBL 301 2 1 3 3.2 Fc1ccc2c(c1)nc(CC(F)(F)F)n2C1CCNCC1 10.1016/j.bmc.2012.09.013
CHEMBL2159765 81493 None 0 Human Binding pKi = 7 7.0 - 1
Inhibition of CCR3 receptorInhibition of CCR3 receptor
ChEMBL 301 2 1 3 3.2 Fc1ccc2c(c1)nc(CC(F)(F)F)n2C1CCNCC1 10.1016/j.bmc.2012.09.013
44389678 123391 None 0 Human Binding pKi = 6 6.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 574 6 1 5 4.6 CS(=O)(=O)N[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL361620 123391 None 0 Human Binding pKi = 6 6.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 574 6 1 5 4.6 CS(=O)(=O)N[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44389669 62617 None 0 Human Binding pKi = 7.0 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178286 62617 None 0 Human Binding pKi = 7.0 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmcl.2005.01.016
44401055 68704 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 454 7 2 4 4.6 COc1ccc(C(CNC(=O)Nc2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL192162 68704 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 454 7 2 4 4.6 COc1ccc(C(CNC(=O)Nc2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401192 70609 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 529 7 1 3 6.4 CC(C)(C)c1ccc(C(CNC(=O)Cc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194943 70609 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 529 7 1 3 6.4 CC(C)(C)c1ccc(C(CNC(=O)Cc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401227 135310 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 421 9 1 4 4.5 COc1ccc(C(CNCCc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL372496 135310 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 421 9 1 4 4.5 COc1ccc(C(CNCCc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401173 69883 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 466 8 2 5 4.5 COc1ccc(NC(=O)NCC(c2ccccc2OC)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193871 69883 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 466 8 2 5 4.5 COc1ccc(NC(=O)NCC(c2ccccc2OC)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44400953 69303 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 488 6 2 3 5.8 Cc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL192751 69303 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 488 6 2 3 5.8 Cc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401108 69848 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 420 5 2 3 4.1 Cc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(C)CC2)cc1 10.1021/jm040827u
CHEMBL193732 69848 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 420 5 2 3 4.1 Cc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(C)CC2)cc1 10.1021/jm040827u
44401062 70072 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 502 9 1 4 5.6 CN(C)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193975 70072 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 502 9 1 4 5.6 CN(C)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721204 116108 None 0 Human Binding pKi = 8.0 8.0 5 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 532 9 3 2 6.7 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)[nH]c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355964 116108 None 0 Human Binding pKi = 8.0 8.0 5 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 532 9 3 2 6.7 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)[nH]c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
11477767 63047 None 0 Human Binding pKi = 8.0 8.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178818 63047 None 0 Human Binding pKi = 8.0 8.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44391171 131864 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 294 1 0 2 4.7 Clc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL369351 131864 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 294 1 0 2 4.7 Clc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
25024650 116104 None 0 Mouse Binding pKi = 7.0 7.0 -21 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2014.11.063
CHEMBL3355960 116104 None 0 Mouse Binding pKi = 7.0 7.0 -21 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2014.11.063
118721203 116107 None 0 Mouse Binding pKi = 7.0 7.0 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccnc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355963 116107 None 0 Mouse Binding pKi = 7.0 7.0 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccnc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)c1 10.1016/j.bmcl.2014.11.063
118721194 116088 None 0 Rat Binding pKi = 6.0 6.0 -229 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.4 COC(C)c1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355944 116088 None 0 Rat Binding pKi = 6.0 6.0 -229 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.4 COC(C)c1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
25024651 116100 None 0 Rat Binding pKi = 6.0 6.0 -69 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355956 116100 None 0 Rat Binding pKi = 6.0 6.0 -69 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
44389719 63040 None 0 Human Binding pKi = 7.0 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 408 5 0 2 4.6 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178771 63040 None 0 Human Binding pKi = 7.0 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 408 5 0 2 4.6 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44389750 166184 None 0 Human Binding pKi = 7.0 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 469 4 1 2 6.0 O=C(c1cccc2[nH]ccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL425875 166184 None 0 Human Binding pKi = 7.0 7.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 469 4 1 2 6.0 O=C(c1cccc2[nH]ccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44401247 69447 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 492 6 2 3 5.7 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(F)cc1 10.1021/jm040827u
CHEMBL193332 69447 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 492 6 2 3 5.7 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(F)cc1 10.1021/jm040827u
44401111 68429 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 480 6 2 3 5.9 CC(C)(C)c1ccc(C(CNC(=O)Nc2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL191719 68429 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 480 6 2 3 5.9 CC(C)(C)c1ccc(C(CNC(=O)Nc2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44400945 71147 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 455 7 1 3 5.2 CC(C)(C)c1ccc(C(CNC(=O)Cc2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL195473 71147 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 455 7 1 3 5.2 CC(C)(C)c1ccc(C(CNC(=O)Cc2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44401128 71138 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 462 6 2 3 5.8 CC(C)(C)c1ccc(C(CNC(=O)Nc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL195427 71138 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 462 6 2 3 5.8 CC(C)(C)c1ccc(C(CNC(=O)Nc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44400972 166088 None 0 Human Binding pKi = 4.9 4.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 337 7 1 3 3.1 Cc1ccc(CCNCC(c2ccccc2)N2CCN(C)CC2)cc1 10.1021/jm040827u
CHEMBL425377 166088 None 0 Human Binding pKi = 4.9 4.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 337 7 1 3 3.1 Cc1ccc(CCNCC(c2ccccc2)N2CCN(C)CC2)cc1 10.1021/jm040827u
44401053 71091 None 0 Human Binding pKi = 4.9 4.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 371 8 1 4 3.0 COc1ccc(C(CNCCc2ccc(F)cc2)N2CCN(C)CC2)cc1 10.1021/jm040827u
CHEMBL195197 71091 None 0 Human Binding pKi = 4.9 4.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 371 8 1 4 3.0 COc1ccc(C(CNCCc2ccc(F)cc2)N2CCN(C)CC2)cc1 10.1021/jm040827u
44401255 69879 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.5 COc1ccccc1CCNCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL193850 69879 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.5 COc1ccccc1CCNCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44389674 62653 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 469 4 1 2 6.0 O=C(c1ccc2[nH]ccc2c1)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178367 62653 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 469 4 1 2 6.0 O=C(c1ccc2[nH]ccc2c1)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
71451391 81300 None 0 Human Binding pKi = 7.9 7.9 12 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 472 8 1 4 4.5 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158781 81300 None 0 Human Binding pKi = 7.9 7.9 12 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 472 8 1 4 4.5 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
10005242 81321 None 0 Human Binding pKi = 7.9 7.9 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158819 81321 None 0 Human Binding pKi = 7.9 7.9 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
23102749 82266 None 0 Human Binding pKi = 7.9 7.9 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 6 1 5 4.3 Cc1c(Cl)ccc(OC2CCN(C3CCN(S(=O)(=O)NC(=O)c4ccccc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171016 82266 None 0 Human Binding pKi = 7.9 7.9 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 6 1 5 4.3 Cc1c(Cl)ccc(OC2CCN(C3CCN(S(=O)(=O)NC(=O)c4ccccc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
59295926 84252 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 6 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cnnc2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208435 84252 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 6 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cnnc2ccccc12 10.1016/j.bmcl.2012.09.113
59295914 84118 None 0 Human Binding pKi = 7.9 7.9 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 638 9 4 8 2.2 CC1(O)CN(S(=O)(=O)c2ccc3c(C(=O)NC[C@@H](O)CN4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)c[nH]c(=O)c3c2)C1 10.1016/j.bmcl.2012.09.112
CHEMBL2207655 84118 None 0 Human Binding pKi = 7.9 7.9 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 638 9 4 8 2.2 CC1(O)CN(S(=O)(=O)c2ccc3c(C(=O)NC[C@@H](O)CN4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)c[nH]c(=O)c3c2)C1 10.1016/j.bmcl.2012.09.112
11952525 116102 None 0 Human Binding pKi = 6.9 6.9 21 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 562 10 0 5 8.0 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355958 116102 None 0 Human Binding pKi = 6.9 6.9 21 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 562 10 0 5 8.0 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)cc1 10.1016/j.bmcl.2014.11.063
11952526 116097 None 0 Mouse Binding pKi = 6.9 6.9 -24 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 534 9 1 4 7.5 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355953 116097 None 0 Mouse Binding pKi = 6.9 6.9 -24 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 534 9 1 4 7.5 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
44391160 123355 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 413 1 1 4 5.6 CC(C)(C)c1csc2nc3n(c(=N)c12)CC/C3=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL361430 123355 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 413 1 1 4 5.6 CC(C)(C)c1csc2nc3n(c(=N)c12)CC/C3=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
44401004 70594 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 471 8 1 3 5.5 Fc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL194885 70594 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 471 8 1 3 5.5 Fc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44389699 63939 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 445 4 1 3 5.1 Nc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2005.01.016
CHEMBL180599 63939 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 445 4 1 3 5.1 Nc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2005.01.016
71462102 81319 None 0 Human Binding pKi = 6.9 6.9 -6 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
CHEMBL2158817 81319 None 0 Human Binding pKi = 6.9 6.9 -6 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
71455217 82293 None 0 Human Binding pKi = 6.9 6.9 -3 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171042 82293 None 0 Human Binding pKi = 6.9 6.9 -3 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
17963141 82300 None 0 Human Binding pKi = 6.9 6.9 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 491 5 1 5 4.1 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171049 82300 None 0 Human Binding pKi = 6.9 6.9 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 491 5 1 5 4.1 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
71459825 84234 None 0 Human Binding pKi = 6.9 6.9 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 433 8 2 5 3.9 N#Cc1ccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2012.09.113
CHEMBL2208417 84234 None 0 Human Binding pKi = 6.9 6.9 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 433 8 2 5 3.9 N#Cc1ccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2012.09.113
71463288 84238 None 0 Human Binding pKi = 6.9 6.9 -6 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 441 8 1 5 5.0 COc1cccc(SC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208421 84238 None 0 Human Binding pKi = 6.9 6.9 -6 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 441 8 1 5 5.0 COc1cccc(SC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
44400992 69979 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 6 2 3 5.8 O=C(NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm040827u
CHEMBL193931 69979 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 6 2 3 5.8 O=C(NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm040827u
44389747 169306 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 424 5 0 2 5.1 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL440750 169306 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 424 5 0 2 5.1 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44401135 69675 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 527 8 1 3 6.8 FC(F)(F)c1ccc(C(CNCCc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193507 69675 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 527 8 1 3 6.8 FC(F)(F)c1ccc(C(CNCCc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721187 116080 None 0 Mouse Binding pKi = 6.9 6.9 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(OC)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355936 116080 None 0 Mouse Binding pKi = 6.9 6.9 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(OC)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721188 116081 None 0 Mouse Binding pKi = 5.9 5.9 -2 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C(N)=O)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355937 116081 None 0 Mouse Binding pKi = 5.9 5.9 -2 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C(N)=O)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721200 116098 None 0 Rat Binding pKi = 5.9 5.9 -275 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 558 9 1 6 7.0 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(-c2nnn[nH]2)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355954 116098 None 0 Rat Binding pKi = 5.9 5.9 -275 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 558 9 1 6 7.0 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(-c2nnn[nH]2)cc1 10.1016/j.bmcl.2014.11.063
44401202 70153 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 542 6 2 3 6.5 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm040827u
CHEMBL194025 70153 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 542 6 2 3 6.5 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm040827u
44401183 70177 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 8 1 3 5.5 FC(F)(F)c1ccc(CCNCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194040 70177 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 8 1 3 5.5 FC(F)(F)c1ccc(CCNCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44389709 63726 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 445 4 1 3 5.1 Nc1ccc(C(=O)N2CCC(N3CCC(Cc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2005.01.016
CHEMBL180122 63726 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 445 4 1 3 5.1 Nc1ccc(C(=O)N2CCC(N3CCC(Cc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2005.01.016
44389688 64566 None 0 Human Binding pKi = 7.9 7.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 495 4 0 3 6.3 C[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181460 64566 None 0 Human Binding pKi = 7.9 7.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 495 4 0 3 6.3 C[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44391330 64042 None 0 Human Binding pKi = 6.9 6.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 322 2 0 2 5.5 CCC1C/C(=C\c2ccccc2Cl)C2=Nc3ccccc3CN21 10.1016/j.bmcl.2004.11.039
CHEMBL180721 64042 None 0 Human Binding pKi = 6.9 6.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 322 2 0 2 5.5 CCC1C/C(=C\c2ccccc2Cl)C2=Nc3ccccc3CN21 10.1016/j.bmcl.2004.11.039
44389721 64304 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1nccc2ccccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL180988 64304 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1nccc2ccccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44391276 123019 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 278 1 0 2 4.2 Fc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL360738 123019 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 278 1 0 2 4.2 Fc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
44391297 132556 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 288 2 0 2 4.6 CCc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL369778 132556 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 288 2 0 2 4.6 CCc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
44391307 168415 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 337 2 0 3 4.7 CN(C)c1ccc(/C=C2\CCN3Cc4ccccc4N=C23)c(Cl)c1 10.1016/j.bmcl.2004.11.039
CHEMBL434151 168415 None 0 Human Binding pKi = 5.9 5.9 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 337 2 0 3 4.7 CN(C)c1ccc(/C=C2\CCN3Cc4ccccc4N=C23)c(Cl)c1 10.1016/j.bmcl.2004.11.039
118721191 116084 None 0 Rat Binding pKi = 5.9 5.9 -331 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 444 8 1 3 6.5 COC(C)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355940 116084 None 0 Rat Binding pKi = 5.9 5.9 -331 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 444 8 1 3 6.5 COC(C)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
70790201 129346 None 0 Human Binding pKi = 5.9 5.9 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 440 5 0 4 3.7 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)N(C)c3ccccn3)CC2)ccc1Cl nan
CHEMBL3670803 129346 None 0 Human Binding pKi = 5.9 5.9 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 440 5 0 4 3.7 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)N(C)c3ccccn3)CC2)ccc1Cl nan
44389695 63951 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 424 5 0 2 5.1 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL180651 63951 None 0 Human Binding pKi = 6.9 6.9 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 424 5 0 2 5.1 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44389712 63116 None 0 Human Binding pKi = 6.8 6.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 442 5 0 2 5.3 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)cc3F)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178916 63116 None 0 Human Binding pKi = 6.8 6.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 442 5 0 2 5.3 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)cc3F)CC2)CC1 10.1016/j.bmcl.2005.01.016
44401086 70555 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 6 2 3 5.5 O=C(NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm040827u
CHEMBL194715 70555 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 6 2 3 5.5 O=C(NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm040827u
44401251 69448 None 0 Human Binding pKi = 4.8 4.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 498 7 2 4 5.4 COc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL193334 69448 None 0 Human Binding pKi = 4.8 4.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 498 7 2 4 5.4 COc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
11283679 64383 None 0 Human Binding pKi = 7.8 7.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4cccnc4n3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181273 64383 None 0 Human Binding pKi = 7.8 7.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4cccnc4n3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
17963315 82284 None 0 Human Binding pKi = 7.8 7.8 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 511 5 1 5 4.4 O=C(NS(=O)(=O)c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171033 82284 None 0 Human Binding pKi = 7.8 7.8 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 511 5 1 5 4.4 O=C(NS(=O)(=O)c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
59296109 84245 None 0 Human Binding pKi = 7.8 7.8 12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 500 8 2 6 3.0 CS(=O)(=O)c1ccccc1C(=O)NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208428 84245 None 0 Human Binding pKi = 7.8 7.8 12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 500 8 2 6 3.0 CS(=O)(=O)c1ccccc1C(=O)NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
59296077 84042 None 0 Human Binding pKi = 7.8 7.8 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(S(C)(=O)=O)ccc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207276 84042 None 0 Human Binding pKi = 7.8 7.8 5 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(S(C)(=O)=O)ccc23)CC1 10.1016/j.bmcl.2012.09.112
44400973 127590 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.5 COc1ccc(C(CNC(=O)Nc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL366231 127590 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.5 COc1ccc(C(CNC(=O)Nc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
69260851 81326 None 0 Human Binding pKi = 6.8 6.8 -2 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158824 81326 None 0 Human Binding pKi = 6.8 6.8 -2 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
10143016 82305 None 0 Human Binding pKi = 6.8 6.8 -3 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 6 1 5 4.5 O=C(NS(=O)(=O)Cc1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171215 82305 None 0 Human Binding pKi = 6.8 6.8 -3 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 6 1 5 4.5 O=C(NS(=O)(=O)Cc1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71454365 84235 None 0 Human Binding pKi = 6.8 6.8 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 465 8 2 6 4.6 O[C@@H](CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)COc1ccc2ncsc2c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208418 84235 None 0 Human Binding pKi = 6.8 6.8 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 465 8 2 6 4.6 O[C@@H](CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)COc1ccc2ncsc2c1 10.1016/j.bmcl.2012.09.113
59296073 84239 None 0 Human Binding pKi = 6.8 6.8 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 483 8 2 6 3.0 N#Cc1cccc(S(=O)(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208422 84239 None 0 Human Binding pKi = 6.8 6.8 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 483 8 2 6 3.0 N#Cc1cccc(S(=O)(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
44401172 124258 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 445 10 1 5 4.4 COc1ccccc1CCNCC(c1ccccc1OC)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
CHEMBL363409 124258 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 445 10 1 5 4.4 COc1ccccc1CCNCC(c1ccccc1OC)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
25024651 116100 None 0 Human Binding pKi = 7.8 7.8 39 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355956 116100 None 0 Human Binding pKi = 7.8 7.8 39 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
44391296 65324 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.0 FC(F)(F)c1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL182889 65324 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.0 FC(F)(F)c1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
44389722 64305 None 0 Human Binding pKi = 6.8 6.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 538 5 1 4 5.2 CC(=O)N[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL180989 64305 None 0 Human Binding pKi = 6.8 6.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 538 5 1 4 5.2 CC(=O)N[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44401052 70103 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 496 9 1 4 5.5 CN(C)c1ccc(C(CNCCc2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL193991 70103 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 496 9 1 4 5.5 CN(C)c1ccc(C(CNCCc2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
56967062 129359 None 0 Human Binding pKi = 7.8 7.8 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 531 6 1 5 4.0 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)n1 nan
CHEMBL3670816 129359 None 0 Human Binding pKi = 7.8 7.8 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 531 6 1 5 4.0 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)n1 nan
44391318 65723 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.3 Clc1ccc(/C=C2\CCN3Cc4ccccc4N=C23)c(Cl)c1 10.1016/j.bmcl.2004.11.039
CHEMBL183441 65723 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.3 Clc1ccc(/C=C2\CCN3Cc4ccccc4N=C23)c(Cl)c1 10.1016/j.bmcl.2004.11.039
118721199 116093 None 0 Rat Binding pKi = 5.8 5.8 2 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 440 8 2 3 5.9 CCc1[nH]c2cc(C(=O)O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355949 116093 None 0 Rat Binding pKi = 5.8 5.8 2 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 440 8 2 3 5.9 CCc1[nH]c2cc(C(=O)O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
25024650 116104 None 0 Rat Binding pKi = 5.8 5.8 -338 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2014.11.063
CHEMBL3355960 116104 None 0 Rat Binding pKi = 5.8 5.8 -338 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2014.11.063
44401235 69864 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.5 COc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193810 69864 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.5 COc1ccc(NC(=O)NCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44400995 71123 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 505 7 2 4 5.9 CN(C)c1ccc(NC(=O)NCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL195353 71123 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 505 7 2 4 5.9 CN(C)c1ccc(NC(=O)NCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401188 69839 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 428 9 1 4 4.4 CN(C)c1ccc(CCNCC(c2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL193656 69839 None 0 Human Binding pKi = 5.8 5.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 428 9 1 4 4.4 CN(C)c1ccc(CCNCC(c2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44401047 71154 None 0 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 462 7 2 3 5.7 Cc1ccc(NC(=O)NCC(CC(C)C)N2CCN(c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/jm040827u
CHEMBL195495 71154 None 0 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 462 7 2 3 5.7 Cc1ccc(NC(=O)NCC(CC(C)C)N2CCN(c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/jm040827u
118721190 116083 None 0 Mouse Binding pKi = 7.8 7.8 5 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 416 7 2 3 5.3 OCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355939 116083 None 0 Mouse Binding pKi = 7.8 7.8 5 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 416 7 2 3 5.3 OCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
11214422 123728 None 0 Human Binding pKi = 7.8 7.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3cccc4cccnc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL362040 123728 None 0 Human Binding pKi = 7.8 7.8 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3cccc4cccnc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44391258 122460 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.3 Clc1cccc(Cl)c1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL360075 122460 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.3 Clc1cccc(Cl)c1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
67114884 129345 None 0 Human Binding pKi = 7.7 7.7 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 6 1 6 3.1 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N4CCOCC4)ccn3)CC2)ccc1Cl nan
CHEMBL3670802 129345 None 0 Human Binding pKi = 7.7 7.7 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 6 1 6 3.1 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N4CCOCC4)ccn3)CC2)ccc1Cl nan
71072115 81289 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 515 8 1 5 5.1 N#Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158770 81289 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 515 8 1 5 5.1 N#Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71072081 81292 None 0 Human Binding pKi = 7.7 7.7 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158773 81292 None 0 Human Binding pKi = 7.7 7.7 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71072113 81293 None 0 Human Binding pKi = 7.7 7.7 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158774 81293 None 0 Human Binding pKi = 7.7 7.7 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
11444350 81296 None 0 Human Binding pKi = 7.7 7.7 7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 558 8 1 4 6.3 O=C(O)[C@H](Cc1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158777 81296 None 0 Human Binding pKi = 7.7 7.7 7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 558 8 1 4 6.3 O=C(O)[C@H](Cc1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71449584 81327 None 0 Human Binding pKi = 7.7 7.7 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158825 81327 None 0 Human Binding pKi = 7.7 7.7 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
69347719 81334 None 0 Human Binding pKi = 7.7 7.7 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccccc1CN1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158831 81334 None 0 Human Binding pKi = 7.7 7.7 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccccc1CN1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71460419 81341 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccc(Cl)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158838 81341 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccc(Cl)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
17963334 82289 None 0 Human Binding pKi = 7.7 7.7 2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171038 82289 None 0 Human Binding pKi = 7.7 7.7 2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
59296064 84240 None 0 Human Binding pKi = 7.7 7.7 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 447 7 2 5 3.5 N#Cc1cccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208423 84240 None 0 Human Binding pKi = 7.7 7.7 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 447 7 2 5 3.5 N#Cc1cccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59295960 84131 None 0 Human Binding pKi = 7.7 7.7 12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 532 8 4 6 2.6 NC(=O)c1c(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207667 84131 None 0 Human Binding pKi = 7.7 7.7 12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 532 8 4 6 2.6 NC(=O)c1c(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.09.112
118721197 116091 None 0 Human Binding pKi = 6.7 6.7 19 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(OC)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355947 116091 None 0 Human Binding pKi = 6.7 6.7 19 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(OC)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44389730 64619 None 0 Human Binding pKi = 6.7 6.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 442 5 0 2 5.3 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)c(F)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL181678 64619 None 0 Human Binding pKi = 6.7 6.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 442 5 0 2 5.3 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)c(F)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
70790198 129339 None 0 Human Binding pKi = 6.7 6.7 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 454 6 1 4 4.2 CCc1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670795 129339 None 0 Human Binding pKi = 6.7 6.7 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 454 6 1 4 4.2 CCc1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
44401056 69870 None 0 Human Binding pKi = 5.7 5.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 492 7 2 4 5.8 COc1ccc(NC(=O)NCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193827 69870 None 0 Human Binding pKi = 5.7 5.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 492 7 2 4 5.8 COc1ccc(NC(=O)NCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
71462389 82275 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 5 1 4 4.8 O=C(O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171024 82275 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 5 1 4 4.8 O=C(O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
71462390 82277 None 0 Human Binding pKi = 6.7 6.7 -6 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 500 5 1 6 4.3 O=C(c1ccc(-c2nn[nH]n2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171026 82277 None 0 Human Binding pKi = 6.7 6.7 -6 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 500 5 1 6 4.3 O=C(c1ccc(-c2nn[nH]n2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
59296114 84242 None 0 Human Binding pKi = 6.7 6.7 -12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 480 7 2 6 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cn2cc(F)ccc2n1 10.1016/j.bmcl.2012.09.113
CHEMBL2208425 84242 None 0 Human Binding pKi = 6.7 6.7 -12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 480 7 2 6 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cn2cc(F)ccc2n1 10.1016/j.bmcl.2012.09.113
67114949 129353 None 0 Human Binding pKi = 8.6 8.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 7 1 5 4.4 Cc1cc(C(=O)N(C)C(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670810 129353 None 0 Human Binding pKi = 8.6 8.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 7 1 5 4.4 Cc1cc(C(=O)N(C)C(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
56967064 129363 None 0 Human Binding pKi = 8.6 8.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 7 1 5 4.2 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)cc(C4CC4)n3)CC2)ccc1Cl nan
CHEMBL3670820 129363 None 0 Human Binding pKi = 8.6 8.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 7 1 5 4.2 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)cc(C4CC4)n3)CC2)ccc1Cl nan
59295939 84247 None 0 Human Binding pKi = 8.6 8.6 12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 461 7 3 4 4.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208430 84247 None 0 Human Binding pKi = 8.6 8.6 12 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 461 7 3 4 4.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
59296000 84249 None 0 Human Binding pKi = 8.6 8.6 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 478 6 3 6 3.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)n1c(=O)[nH]c2ccccc21 10.1016/j.bmcl.2012.09.113
CHEMBL2208432 84249 None 0 Human Binding pKi = 8.6 8.6 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 478 6 3 6 3.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)n1c(=O)[nH]c2ccccc21 10.1016/j.bmcl.2012.09.113
59296104 84250 None 0 Human Binding pKi = 8.6 8.6 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 503 7 2 5 3.8 CN(C[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C(=O)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208433 84250 None 0 Human Binding pKi = 8.6 8.6 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 503 7 2 5 3.8 CN(C[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C(=O)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
59295974 84136 None 0 Human Binding pKi = 8.6 8.6 19 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4cc(S(C)(=O)=O)ccc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207672 84136 None 0 Human Binding pKi = 8.6 8.6 19 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4cc(S(C)(=O)=O)ccc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
11179794 64314 None 0 Human Binding pKi = 7.7 7.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3nccc4ccccc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181034 64314 None 0 Human Binding pKi = 7.7 7.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3nccc4ccccc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44389770 123888 None 0 Human Binding pKi = 6.7 6.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 552 6 1 4 5.5 CC(=O)NC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL362401 123888 None 0 Human Binding pKi = 6.7 6.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 552 6 1 4 5.5 CC(=O)NC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44400954 127123 None 0 Human Binding pKi = 5.7 5.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 518 6 2 3 7.1 CC(C)(C)c1ccc(NC(=O)NCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL365584 127123 None 0 Human Binding pKi = 5.7 5.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 518 6 2 3 7.1 CC(C)(C)c1ccc(NC(=O)NCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721186 116079 None 0 Mouse Binding pKi = 6.7 6.7 -2 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(O)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355935 116079 None 0 Mouse Binding pKi = 6.7 6.7 -2 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(O)cc2)CC1 10.1016/j.bmcl.2014.11.063
44400982 71149 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 9 1 4 5.8 COc1ccccc1CCNCC(c1ccc(C(C)(C)C)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL195480 71149 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 9 1 4 5.8 COc1ccccc1CCNCC(c1ccc(C(C)(C)C)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44401252 70840 None 0 Human Binding pKi = 4.7 4.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 323 7 1 3 2.8 CN1CCN(C(CNCCc2ccccc2)c2ccccc2)CC1 10.1021/jm040827u
CHEMBL195093 70840 None 0 Human Binding pKi = 4.7 4.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 323 7 1 3 2.8 CN1CCN(C(CNCCc2ccccc2)c2ccccc2)CC1 10.1021/jm040827u
44401225 69982 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 515 8 1 3 7.1 CC(C)(C)c1ccc(C(CNCCc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193938 69982 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 515 8 1 3 7.1 CC(C)(C)c1ccc(C(CNCCc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401067 168528 None 0 Human Binding pKi = 5.7 5.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 450 7 2 4 4.8 COc1ccc(C(CNC(=O)Nc2ccc(C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL434918 168528 None 0 Human Binding pKi = 5.7 5.7 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 450 7 2 4 4.8 COc1ccc(C(CNC(=O)Nc2ccc(C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44389690 64688 None 0 Human Binding pKi = 5.7 5.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 426 5 0 2 4.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL181827 64688 None 0 Human Binding pKi = 5.7 5.7 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 426 5 0 2 4.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
11386642 63110 None 0 Human Binding pKi = 7.6 7.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 507 5 0 3 6.5 C=C[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178887 63110 None 0 Human Binding pKi = 7.6 7.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 507 5 0 3 6.5 C=C[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
56966925 129335 None 0 Human Binding pKi = 7.6 7.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 483 6 2 5 3.0 CNC(=O)c1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670791 129335 None 0 Human Binding pKi = 7.6 7.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 483 6 2 5 3.0 CNC(=O)c1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
24937092 116101 None 0 Mouse Binding pKi = 6.6 6.6 -2 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 500 10 0 5 6.4 CCOC(=O)Cn1c(CC)c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2014.11.063
CHEMBL3355957 116101 None 0 Mouse Binding pKi = 6.6 6.6 -2 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 500 10 0 5 6.4 CCOC(=O)Cn1c(CC)c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2014.11.063
118721186 116079 None 0 Rat Binding pKi = 5.6 5.6 -29 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(O)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355935 116079 None 0 Rat Binding pKi = 5.6 5.6 -29 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(O)cc2)CC1 10.1016/j.bmcl.2014.11.063
44401109 71105 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 515 8 1 3 6.8 CC(C)(C)c1ccc(C(CNCCc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL195293 71105 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 515 8 1 3 6.8 CC(C)(C)c1ccc(C(CNCCc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
56966998 129357 None 0 Human Binding pKi = 6.6 6.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 527 7 1 6 3.3 COc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670814 129357 None 0 Human Binding pKi = 6.6 6.6 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 527 7 1 6 3.3 COc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
118721194 116088 None 0 Mouse Binding pKi = 7.6 7.6 -5 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.4 COC(C)c1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355944 116088 None 0 Mouse Binding pKi = 7.6 7.6 -5 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.4 COC(C)c1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
71460416 81295 None 0 Human Binding pKi = 7.6 7.6 2 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 520 9 1 5 5.3 COc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158776 81295 None 0 Human Binding pKi = 7.6 7.6 2 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 520 9 1 5 5.3 COc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
71456725 81329 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158827 81329 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
71072057 81343 None 0 Human Binding pKi = 7.6 7.6 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1cccc(F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158840 81343 None 0 Human Binding pKi = 7.6 7.6 5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1cccc(F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
17963332 82291 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 541 6 1 6 4.4 COc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171040 82291 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 541 6 1 6 4.4 COc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963153 82297 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171046 82297 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
59295982 84048 None 0 Human Binding pKi = 7.6 7.6 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 568 8 4 7 2.1 NS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207282 84048 None 0 Human Binding pKi = 7.6 7.6 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 568 8 4 7 2.1 NS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
44391331 64855 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 394 4 0 2 6.3 CCCCC1C/C(=C\c2ccccc2Br)C2=Nc3ccccc3CN21 10.1016/j.bmcl.2004.11.039
CHEMBL181984 64855 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 394 4 0 2 6.3 CCCCC1C/C(=C\c2ccccc2Br)C2=Nc3ccccc3CN21 10.1016/j.bmcl.2004.11.039
44389698 64391 None 0 Human Binding pKi = 6.6 6.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(Cl)ccc3Cl)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL181290 64391 None 0 Human Binding pKi = 6.6 6.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(Cl)ccc3Cl)CC2)CC1 10.1016/j.bmcl.2005.01.016
69347980 81335 None 0 Human Binding pKi = 6.6 6.6 -5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)c1cccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158832 81335 None 0 Human Binding pKi = 6.6 6.6 -5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)c1cccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71458869 82273 None 0 Human Binding pKi = 6.6 6.6 -2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 506 7 1 5 4.6 O=C(O)COc1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171022 82273 None 0 Human Binding pKi = 6.6 6.6 -2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 506 7 1 5 4.6 O=C(O)COc1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
71449857 82274 None 0 Human Binding pKi = 6.6 6.6 -10 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 5 1 4 4.8 O=C(O)c1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171023 82274 None 0 Human Binding pKi = 6.6 6.6 -10 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 5 1 4 4.8 O=C(O)c1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71463287 84236 None 0 Human Binding pKi = 6.6 6.6 -79 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 420 7 1 5 4.1 N#Cc1cccc(OC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208419 84236 None 0 Human Binding pKi = 6.6 6.6 -79 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 420 7 1 5 4.1 N#Cc1cccc(OC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59296085 84243 None 0 Human Binding pKi = 6.6 6.6 -2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 506 8 2 7 3.1 CS(=O)(=O)c1ccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2012.09.113
CHEMBL2208426 84243 None 0 Human Binding pKi = 6.6 6.6 -2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 506 8 2 7 3.1 CS(=O)(=O)c1ccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2012.09.113
71458870 82282 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 5 1 4 5.2 Cc1ccc(C(=O)N2CCC(N3CC[C@@H](Oc4ccc(Cl)c(C)c4Cl)C[C@H]3C(=O)O)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171031 82282 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 5 1 4 5.2 Cc1ccc(C(=O)N2CCC(N3CC[C@@H](Oc4ccc(Cl)c(C)c4Cl)C[C@H]3C(=O)O)CC2)cc1 10.1016/j.bmcl.2012.08.124
44389832 63945 None 0 Human Binding pKi = 7.6 7.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccnc4ccccc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL180621 63945 None 0 Human Binding pKi = 7.6 7.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccnc4ccccc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44391176 122677 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 385 1 1 4 4.9 Cc1sc2nc3n(c(=N)c2c1C)CC/C3=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL360268 122677 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 385 1 1 4 4.9 Cc1sc2nc3n(c(=N)c2c1C)CC/C3=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
57718837 116076 None 0 Rat Binding pKi = 6.6 6.6 -45 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 414 7 1 2 6.4 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355932 116076 None 0 Rat Binding pKi = 6.6 6.6 -45 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 414 7 1 2 6.4 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721189 116082 None 0 Rat Binding pKi = 6.6 6.6 -7 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 400 6 1 2 6.1 Cc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355938 116082 None 0 Rat Binding pKi = 6.6 6.6 -7 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 400 6 1 2 6.1 Cc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
11952524 116095 None 0 Rat Binding pKi = 6.6 6.6 -3 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 490 8 0 3 7.8 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccccc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355951 116095 None 0 Rat Binding pKi = 6.6 6.6 -3 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 490 8 0 3 7.8 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccccc1 10.1016/j.bmcl.2014.11.063
11952525 116102 None 0 Mouse Binding pKi = 5.6 5.6 -21 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 562 10 0 5 8.0 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355958 116102 None 0 Mouse Binding pKi = 5.6 5.6 -21 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 562 10 0 5 8.0 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)cc1 10.1016/j.bmcl.2014.11.063
118721201 116099 None 0 Rat Binding pKi = 5.6 5.6 2 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 548 10 1 4 7.6 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355955 116099 None 0 Rat Binding pKi = 5.6 5.6 2 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 548 10 1 4 7.6 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
44389688 64566 None 0 Human Binding pKi = 6.6 6.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 495 4 0 3 6.3 C[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181460 64566 None 0 Human Binding pKi = 6.6 6.6 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 495 4 0 3 6.3 C[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44401117 70229 None 0 Human Binding pKi = 4.6 4.6 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 413 7 1 3 4.2 Cc1ccc(CC(=O)NCC(c2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL194070 70229 None 0 Human Binding pKi = 4.6 4.6 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 413 7 1 3 4.2 Cc1ccc(CC(=O)NCC(c2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44391277 65807 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 369 1 1 4 4.4 Cc1oc2nc3n(c(=N)c2c1C)CC/C3=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL183478 65807 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 369 1 1 4 4.4 Cc1oc2nc3n(c(=N)c2c1C)CC/C3=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
118721205 116109 None 0 Mouse Binding pKi = 6.6 6.6 -67 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 653 11 3 5 7.2 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)O)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355965 116109 None 0 Mouse Binding pKi = 6.6 6.6 -67 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 653 11 3 5 7.2 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)O)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
44391236 123190 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 357 1 1 4 4.3 N=c1c2ccsc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL361149 123190 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 357 1 1 4 4.3 N=c1c2ccsc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
11360133 123387 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 351 1 1 3 4.2 N=c1c2ccccc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL361606 123387 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 351 1 1 3 4.2 N=c1c2ccccc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
44389704 62523 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 509 5 0 3 6.7 CC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178136 62523 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 509 5 0 3 6.7 CC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44391252 65865 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 397 2 1 4 5.2 N=c1c2c(C3CC3)csc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL183520 65865 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 397 2 1 4 5.2 N=c1c2c(C3CC3)csc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
44391317 65523 None 0 Human Binding pKi = 5.5 5.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 336 2 0 2 5.7 C(=C1\CCN2Cc3ccccc3N=C12)\c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.11.039
CHEMBL183052 65523 None 0 Human Binding pKi = 5.5 5.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 336 2 0 2 5.7 C(=C1\CCN2Cc3ccccc3N=C12)\c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.11.039
44400990 166346 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 454 7 2 3 5.5 CC(C)CC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL426822 166346 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 454 7 2 3 5.5 CC(C)CC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
11466397 62899 None 0 Rat Binding pKi = 5.5 5.5 -407 4
In vitro binding affinity against rat CC chemokine receptor 3In vitro binding affinity against rat CC chemokine receptor 3
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178447 62899 None 0 Rat Binding pKi = 5.5 5.5 -407 4
In vitro binding affinity against rat CC chemokine receptor 3In vitro binding affinity against rat CC chemokine receptor 3
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
71451392 81305 None 0 Human Binding pKi = 8.5 8.5 31 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 C[C@](Cc1ccccc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158786 81305 None 0 Human Binding pKi = 8.5 8.5 31 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 C[C@](Cc1ccccc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71458868 82264 None 0 Human Binding pKi = 8.5 8.5 6 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 568 6 1 6 4.8 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)NS(=O)(=O)c4ccc(N(C)C)cc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171014 82264 None 0 Human Binding pKi = 8.5 8.5 6 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 568 6 1 6 4.8 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)NS(=O)(=O)c4ccc(N(C)C)cc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
59295958 84046 None 0 Human Binding pKi = 8.5 8.5 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccc(F)cc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207280 84046 None 0 Human Binding pKi = 8.5 8.5 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccc(F)cc12 10.1016/j.bmcl.2012.09.112
59296100 84122 None 0 Human Binding pKi = 8.5 8.5 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 460 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]nc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207659 84122 None 0 Human Binding pKi = 8.5 8.5 7 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 460 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]nc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
59296090 84126 None 0 Human Binding pKi = 8.5 8.5 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.3 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)cc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
CHEMBL2207662 84126 None 0 Human Binding pKi = 8.5 8.5 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 507 7 3 5 3.3 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)cc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
10653 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C nan
59534386 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C nan
CHEMBL3670800 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C nan
DB15269 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C nan
11466397 62899 None 0 Human Binding pKi = 8.5 8.5 -1 4
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178447 62899 None 0 Human Binding pKi = 8.5 8.5 -1 4
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
11466397 62899 None 0 Human Binding pKi = 8.5 8.5 -1 4
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178447 62899 None 0 Human Binding pKi = 8.5 8.5 -1 4
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
56966926 129347 None 0 Human Binding pKi = 8.5 8.5 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 8 2 5 4.1 Cc1cc(C(=O)NCC2CC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670804 129347 None 0 Human Binding pKi = 8.5 8.5 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 8 2 5 4.1 Cc1cc(C(=O)NCC2CC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
71072104 81294 None 0 Human Binding pKi = 8.4 8.4 15 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 520 9 1 5 5.3 COc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158775 81294 None 0 Human Binding pKi = 8.4 8.4 15 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 520 9 1 5 5.3 COc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
66615678 81299 None 0 Human Binding pKi = 8.4 8.4 19 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 488 8 1 4 5.0 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158780 81299 None 0 Human Binding pKi = 8.4 8.4 19 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 488 8 1 4 5.0 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
59296039 84244 None 0 Human Binding pKi = 8.4 8.4 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 467 8 3 6 3.2 COc1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)ccc1N 10.1016/j.bmcl.2012.09.113
CHEMBL2208427 84244 None 0 Human Binding pKi = 8.4 8.4 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 467 8 3 6 3.2 COc1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)ccc1N 10.1016/j.bmcl.2012.09.113
59295984 84045 None 0 Human Binding pKi = 8.4 8.4 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(F)ccc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207279 84045 None 0 Human Binding pKi = 8.4 8.4 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(F)ccc23)CC1 10.1016/j.bmcl.2012.09.112
59296048 84050 None 0 Human Binding pKi = 8.4 8.4 6 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 582 9 4 7 2.4 CNS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207284 84050 None 0 Human Binding pKi = 8.4 8.4 6 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 582 9 4 7 2.4 CNS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
59295969 84051 None 0 Human Binding pKi = 8.4 8.4 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 608 10 4 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NC3CC3)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207285 84051 None 0 Human Binding pKi = 8.4 8.4 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 608 10 4 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NC3CC3)ccc12 10.1016/j.bmcl.2012.09.112
71454296 84129 None 0 Human Binding pKi = 8.4 8.4 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 521 7 2 6 3.3 Cn1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c(C(F)(F)F)cc1=O 10.1016/j.bmcl.2012.09.112
CHEMBL2207665 84129 None 0 Human Binding pKi = 8.4 8.4 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 521 7 2 6 3.3 Cn1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c(C(F)(F)F)cc1=O 10.1016/j.bmcl.2012.09.112
59296094 84133 None 0 Human Binding pKi = 8.4 8.4 31 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 480 7 3 6 2.7 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207669 84133 None 0 Human Binding pKi = 8.4 8.4 31 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 480 7 3 6 2.7 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1Cl 10.1016/j.bmcl.2012.09.112
44389737 123929 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1ccc2ncccc2c1)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL362649 123929 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1ccc2ncccc2c1)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
66906657 116086 None 0 Human Binding pKi = 7.5 7.5 12 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355942 116086 None 0 Human Binding pKi = 7.5 7.5 12 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
68849581 81320 None 0 Human Binding pKi = 7.5 7.5 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
CHEMBL2158818 81320 None 0 Human Binding pKi = 7.5 7.5 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
69348078 81322 None 0 Human Binding pKi = 7.5 7.5 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)[C@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158820 81322 None 0 Human Binding pKi = 7.5 7.5 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)[C@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
69272932 81330 None 0 Human Binding pKi = 7.5 7.5 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158828 81330 None 0 Human Binding pKi = 7.5 7.5 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072034 81339 None 0 Human Binding pKi = 7.5 7.5 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 490 8 1 4 5.2 O=C(O)[C@@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158836 81339 None 0 Human Binding pKi = 7.5 7.5 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 490 8 1 4 5.2 O=C(O)[C@@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
17963208 82285 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 529 5 1 5 4.5 O=C(NS(=O)(=O)c1ccc(F)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171034 82285 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 529 5 1 5 4.5 O=C(NS(=O)(=O)c1ccc(F)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71453505 82292 None 0 Human Binding pKi = 7.5 7.5 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 554 6 1 6 4.5 CN(C)c1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171041 82292 None 0 Human Binding pKi = 7.5 7.5 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 554 6 1 6 4.5 CN(C)c1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963347 82296 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 579 5 1 5 5.4 O=C(NS(=O)(=O)c1cccc(C(F)(F)F)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171045 82296 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 579 5 1 5 5.4 O=C(NS(=O)(=O)c1cccc(C(F)(F)F)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71452601 84241 None 0 Human Binding pKi = 7.5 7.5 -100 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 434 8 1 5 4.5 N#Cc1cccc(OC[C@@H](O)CCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208424 84241 None 0 Human Binding pKi = 7.5 7.5 -100 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 434 8 1 5 4.5 N#Cc1cccc(OC[C@@H](O)CCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59296098 84132 None 0 Human Binding pKi = 7.5 7.5 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 446 7 3 6 2.0 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1 10.1016/j.bmcl.2012.09.112
CHEMBL2207668 84132 None 0 Human Binding pKi = 7.5 7.5 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 446 7 3 6 2.0 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1 10.1016/j.bmcl.2012.09.112
44391213 122930 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 365 1 0 3 4.3 C/N=c1/c2ccccc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL360560 122930 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 365 1 0 3 4.3 C/N=c1/c2ccccc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
118721198 116092 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(C(N)=O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355948 116092 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(C(N)=O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44401177 68422 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 490 9 1 4 5.9 CN(C)c1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL191693 68422 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 490 9 1 4 5.9 CN(C)c1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401182 71093 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 476 7 2 3 6.0 Cc1cc(C)cc(NC(=O)NCC(CC(C)C)N2CCN(c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/jm040827u
CHEMBL195202 71093 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 476 7 2 3 6.0 Cc1cc(C)cc(NC(=O)NCC(CC(C)C)N2CCN(c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/jm040827u
25056325 71201 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 496 7 2 3 6.5 Cc1ccc(NC(=O)NCC(c2ccc(-c3ccccc3)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL195610 71201 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 496 7 2 3 6.5 Cc1ccc(NC(=O)NCC(c2ccc(-c3ccccc3)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
136229178 82276 None 0 Human Binding pKi = 6.5 6.5 -19 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 516 5 1 6 4.5 O=C(c1ccc(-c2noc(=O)[nH]2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171025 82276 None 0 Human Binding pKi = 6.5 6.5 -19 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 516 5 1 6 4.5 O=C(c1ccc(-c2noc(=O)[nH]2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71452602 84253 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 433 8 2 5 3.9 N#Cc1cccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208436 84253 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 433 8 2 5 3.9 N#Cc1cccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
118721185 116078 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355934 116078 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721204 116108 None 0 Rat Binding pKi = 6.5 6.5 -28 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 532 9 3 2 6.7 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)[nH]c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355964 116108 None 0 Rat Binding pKi = 6.5 6.5 -28 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 532 9 3 2 6.7 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)[nH]c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
44391329 122406 None 0 Human Binding pKi = 5.5 5.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 344 2 0 3 4.9 FC(F)(F)Oc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL359918 122406 None 0 Human Binding pKi = 5.5 5.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 344 2 0 3 4.9 FC(F)(F)Oc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
11477767 63047 None 0 Human Binding pKi = 6.5 6.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178818 63047 None 0 Human Binding pKi = 6.5 6.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44400948 71095 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 510 7 2 3 6.8 Cc1cc(C)cc(NC(=O)NCC(c2ccc(-c3ccccc3)cc2)N2CCN(C3CCCCC3)CC2)c1 10.1021/jm040827u
CHEMBL195214 71095 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 510 7 2 3 6.8 Cc1cc(C)cc(NC(=O)NCC(c2ccc(-c3ccccc3)cc2)N2CCN(C3CCCCC3)CC2)c1 10.1021/jm040827u
118721189 116082 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 400 6 1 2 6.1 Cc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355938 116082 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 400 6 1 2 6.1 Cc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44389738 64492 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 525 6 0 4 6.1 CCO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181379 64492 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 525 6 0 4 6.1 CCO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
118721206 116110 None 0 Rat Binding pKi = 5.5 5.5 -97 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 667 11 2 6 7.3 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)OC)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355966 116110 None 0 Rat Binding pKi = 5.5 5.5 -97 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 667 11 2 6 7.3 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)OC)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
44389868 64660 None 0 Human Binding pKi = 6.5 6.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 588 7 1 5 4.9 CS(=O)(=O)NC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181789 64660 None 0 Human Binding pKi = 6.5 6.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 588 7 1 5 4.9 CS(=O)(=O)NC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44401160 69487 None 0 Human Binding pKi = 5.5 5.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 436 6 2 4 3.8 COc1ccccc1NC(=O)NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C)CC1 10.1021/jm040827u
CHEMBL193369 69487 None 0 Human Binding pKi = 5.5 5.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 436 6 2 4 3.8 COc1ccccc1NC(=O)NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C)CC1 10.1021/jm040827u
118721206 116110 None 0 Human Binding pKi = 7.5 7.5 19 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 667 11 2 6 7.3 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)OC)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355966 116110 None 0 Human Binding pKi = 7.5 7.5 19 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 667 11 2 6 7.3 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)OC)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
44389784 64346 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3cnc4ccccc4n3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181137 64346 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3cnc4ccccc4n3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44401083 124606 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.8 COc1ccccc1C(CNCCc1cc(Cl)cc(Cl)c1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL364047 124606 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.8 COc1ccccc1C(CNCCc1cc(Cl)cc(Cl)c1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44401154 70288 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 9 1 4 5.8 COc1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194161 70288 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 9 1 4 5.8 COc1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401031 70057 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 503 8 1 3 7.1 CC(C)(C)c1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193973 70057 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 503 8 1 3 7.1 CC(C)(C)c1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401011 135309 None 0 Human Binding pKi = 4.5 4.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 510 8 1 4 5.0 CN(C)c1ccc(C(CNC(=O)Cc2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL372493 135309 None 0 Human Binding pKi = 4.5 4.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 510 8 1 4 5.0 CN(C)c1ccc(C(CNC(=O)Cc2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44391247 123564 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 307 1 1 3 4.1 N=c1c2ccccc2nc2n1CC/C2=C\c1ccccc1Cl 10.1016/j.bmcl.2004.11.039
CHEMBL361761 123564 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 307 1 1 3 4.1 N=c1c2ccccc2nc2n1CC/C2=C\c1ccccc1Cl 10.1016/j.bmcl.2004.11.039
44389910 63376 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4cnccc4n3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL179490 63376 None 0 Human Binding pKi = 7.5 7.5 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4cnccc4n3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
44391177 64490 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 411 1 1 4 5.2 N=c1c2c3c(sc2nc2n1CC/C2=C\c1ccccc1Br)CCCC3 10.1016/j.bmcl.2004.11.039
CHEMBL181367 64490 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 411 1 1 4 5.2 N=c1c2c3c(sc2nc2n1CC/C2=C\c1ccccc1Br)CCCC3 10.1016/j.bmcl.2004.11.039
44401206 127124 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 447 8 1 3 5.8 CC(C)(C)c1ccc(C(CNCCc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL365596 127124 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 447 8 1 3 5.8 CC(C)(C)c1ccc(C(CNCCc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721205 116109 None 0 Rat Binding pKi = 5.5 5.5 -870 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 653 11 3 5 7.2 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)O)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355965 116109 None 0 Rat Binding pKi = 5.5 5.5 -870 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 653 11 3 5 7.2 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)O)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
44401063 133167 None 0 Human Binding pKi = 5.5 5.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 444 7 2 4 4.7 COc1ccccc1C(CNC(=O)Nc1ccc(C)cc1)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
CHEMBL370244 133167 None 0 Human Binding pKi = 5.5 5.5 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 444 7 2 4 4.7 COc1ccccc1C(CNC(=O)Nc1ccc(C)cc1)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
44391192 63908 None 0 Human Binding pKi = 6.4 6.4 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 301 2 1 3 4.0 CCc1ccccc1/C=C1\CCn2c1nc1ccccc1c2=N 10.1016/j.bmcl.2004.11.039
CHEMBL180446 63908 None 0 Human Binding pKi = 6.4 6.4 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 301 2 1 3 4.0 CCc1ccccc1/C=C1\CCn2c1nc1ccccc1c2=N 10.1016/j.bmcl.2004.11.039
44401248 136068 None 0 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.5 COc1ccccc1NC(=O)NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL373158 136068 None 0 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.5 COc1ccccc1NC(=O)NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
118721189 116082 None 0 Mouse Binding pKi = 7.4 7.4 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 400 6 1 2 6.1 Cc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355938 116082 None 0 Mouse Binding pKi = 7.4 7.4 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 400 6 1 2 6.1 Cc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721196 116090 None 0 Mouse Binding pKi = 6.4 6.4 -4 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355946 116090 None 0 Mouse Binding pKi = 6.4 6.4 -4 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721197 116091 None 0 Rat Binding pKi = 5.4 5.4 -19 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(OC)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355947 116091 None 0 Rat Binding pKi = 5.4 5.4 -19 2
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(OC)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
57718829 116094 None 0 Human Binding pKi = 7.4 7.4 2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 428 7 0 3 6.4 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1C 10.1016/j.bmcl.2014.11.063
CHEMBL3355950 116094 None 0 Human Binding pKi = 7.4 7.4 2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 428 7 0 3 6.4 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1C 10.1016/j.bmcl.2014.11.063
44389752 64129 None 0 Human Binding pKi = 7.4 7.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1ccnc2ccccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL180813 64129 None 0 Human Binding pKi = 7.4 7.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1ccnc2ccccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
118721198 116092 None 0 Mouse Binding pKi = 6.4 6.4 -1 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(C(N)=O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355948 116092 None 0 Mouse Binding pKi = 6.4 6.4 -1 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(C(N)=O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44400950 68689 None 0 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 449 6 2 4 4.2 CN1CCN(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(N(C)C)cc2)CC1 10.1021/jm040827u
CHEMBL192045 68689 None 0 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 449 6 2 4 4.2 CN1CCN(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(N(C)C)cc2)CC1 10.1021/jm040827u
10151756 81317 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.1 O=C(O)C(c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158815 81317 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 462 6 1 4 5.1 O=C(O)C(c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
69274365 81328 None 0 Human Binding pKi = 7.4 7.4 -7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158826 81328 None 0 Human Binding pKi = 7.4 7.4 -7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71449585 81331 None 0 Human Binding pKi = 7.4 7.4 -7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 492 8 1 5 5.2 O=C(O)COc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158829 81331 None 0 Human Binding pKi = 7.4 7.4 -7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 492 8 1 5 5.2 O=C(O)COc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
17963196 82287 None 0 Human Binding pKi = 7.4 7.4 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 541 6 1 6 4.4 COc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171036 82287 None 0 Human Binding pKi = 7.4 7.4 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 541 6 1 6 4.4 COc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
118721202 116106 None 0 Rat Binding pKi = 6.4 6.4 -77 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cc(C(=O)O)ccn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355962 116106 None 0 Rat Binding pKi = 6.4 6.4 -77 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cc(C(=O)O)ccn1 10.1016/j.bmcl.2014.11.063
44391212 65864 None 0 Human Binding pKi = 5.4 5.4 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 303 2 1 4 3.5 COc1ccc(/C=C2\CCn3c2nc2ccccc2c3=N)cc1 10.1016/j.bmcl.2004.11.039
CHEMBL183519 65864 None 0 Human Binding pKi = 5.4 5.4 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 303 2 1 4 3.5 COc1ccc(/C=C2\CCn3c2nc2ccccc2c3=N)cc1 10.1016/j.bmcl.2004.11.039
44401088 166445 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 483 9 1 4 5.4 COc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL427357 166445 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 483 9 1 4 5.4 COc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44389675 62881 None 0 Human Binding pKi = 6.4 6.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 525 6 0 4 6.0 COC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178438 62881 None 0 Human Binding pKi = 6.4 6.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 525 6 0 4 6.0 COC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
71449859 82280 None 0 Human Binding pKi = 6.4 6.4 -10 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 600 10 1 8 5.1 O=C(O)CCCCn1nnc(-c2ccc(C(=O)N3CCC(N4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)CC3)cc2)n1 10.1016/j.bmcl.2012.08.124
CHEMBL2171029 82280 None 0 Human Binding pKi = 6.4 6.4 -10 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 600 10 1 8 5.1 O=C(O)CCCCn1nnc(-c2ccc(C(=O)N3CCC(N4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)CC3)cc2)n1 10.1016/j.bmcl.2012.08.124
71462391 82283 None 0 Human Binding pKi = 6.4 6.4 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 554 6 1 6 3.9 CS(=O)(=O)c1cccc(C(=O)N2CC[C@@H](N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)[C@H](C(=O)O)C2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171032 82283 None 0 Human Binding pKi = 6.4 6.4 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 554 6 1 6 3.9 CS(=O)(=O)c1cccc(C(=O)N2CC[C@@H](N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)[C@H](C(=O)O)C2)c1 10.1016/j.bmcl.2012.08.124
118721205 116109 None 0 Human Binding pKi = 8.4 8.4 67 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 653 11 3 5 7.2 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)O)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355965 116109 None 0 Human Binding pKi = 8.4 8.4 67 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 653 11 3 5 7.2 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)O)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
67115149 129351 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 8 2 5 4.5 CCC(C)NC(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670808 129351 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 8 2 5 4.5 CCC(C)NC(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
68028908 129360 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 7 1 5 4.5 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)cc(C(C)C)n3)CC2)ccc1Cl nan
CHEMBL3670817 129360 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 7 1 5 4.5 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)cc(C(C)C)n3)CC2)ccc1Cl nan
68029259 129354 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 7 2 5 4.2 Cc1cc(C(=O)NC2CCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670811 129354 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 537 7 2 5 4.2 Cc1cc(C(=O)NC2CCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
118721191 116084 None 0 Human Binding pKi = 8.4 8.4 12 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 444 8 1 3 6.5 COC(C)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355940 116084 None 0 Human Binding pKi = 8.4 8.4 12 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 444 8 1 3 6.5 COC(C)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
67115103 129349 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 8 2 5 4.3 Cc1cc(C(=O)NCC(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670806 129349 None 0 Human Binding pKi = 8.4 8.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 539 8 2 5 4.3 Cc1cc(C(=O)NCC(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
56966996 129350 None 0 Human Binding pKi = 8.3 8.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 547 8 2 5 3.9 Cc1cc(C(=O)NCC(F)F)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670807 129350 None 0 Human Binding pKi = 8.3 8.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 547 8 2 5 3.9 Cc1cc(C(=O)NCC(F)F)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
118721200 116098 None 0 Human Binding pKi = 8.3 8.3 15 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 558 9 1 6 7.0 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(-c2nnn[nH]2)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355954 116098 None 0 Human Binding pKi = 8.3 8.3 15 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 558 9 1 6 7.0 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(-c2nnn[nH]2)cc1 10.1016/j.bmcl.2014.11.063
67115023 129344 None 0 Human Binding pKi = 8.3 8.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 523 6 1 5 3.9 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N4CCCC4)ccn3)CC2)ccc1Cl nan
CHEMBL3670801 129344 None 0 Human Binding pKi = 8.3 8.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 523 6 1 5 3.9 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N4CCCC4)ccn3)CC2)ccc1Cl nan
118721194 116088 None 0 Human Binding pKi = 8.3 8.3 5 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 426 8 1 3 6.4 COC(C)c1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355944 116088 None 0 Human Binding pKi = 8.3 8.3 5 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 426 8 1 3 6.4 COC(C)c1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
11952526 116097 None 0 Human Binding pKi = 8.3 8.3 24 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 534 9 1 4 7.5 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355953 116097 None 0 Human Binding pKi = 8.3 8.3 24 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 534 9 1 4 7.5 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
44389744 123940 None 0 Human Binding pKi = 7.4 7.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL362700 123940 None 0 Human Binding pKi = 7.4 7.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
66906657 116086 None 0 Mouse Binding pKi = 6.4 6.4 -12 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355942 116086 None 0 Mouse Binding pKi = 6.4 6.4 -12 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721199 116093 None 0 Human Binding pKi = 5.4 5.4 -2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 440 8 2 3 5.9 CCc1[nH]c2cc(C(=O)O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355949 116093 None 0 Human Binding pKi = 5.4 5.4 -2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 440 8 2 3 5.9 CCc1[nH]c2cc(C(=O)O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721188 116081 None 0 Rat Binding pKi = 5.4 5.4 -8 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C(N)=O)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355937 116081 None 0 Rat Binding pKi = 5.4 5.4 -8 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C(N)=O)cc2)CC1 10.1016/j.bmcl.2014.11.063
44401189 69865 None 0 Human Binding pKi = 4.4 4.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 429 8 1 4 3.9 COc1ccc(C(CNC(=O)Cc2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL193818 69865 None 0 Human Binding pKi = 4.4 4.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 429 8 1 4 3.9 COc1ccc(C(CNC(=O)Cc2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
44391800 64294 None 0 Human Binding pKi = 6.4 6.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 484 6 0 3 4.9 COc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL180939 64294 None 0 Human Binding pKi = 6.4 6.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 484 6 0 3 4.9 COc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44389675 62881 None 0 Human Binding pKi = 7.4 7.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 525 6 0 4 6.0 COC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178438 62881 None 0 Human Binding pKi = 7.4 7.4 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 525 6 0 4 6.0 COC[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
25024850 116105 None 0 Mouse Binding pKi = 6.4 6.4 -6 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1cccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)n1 10.1016/j.bmcl.2014.11.063
CHEMBL3355961 116105 None 0 Mouse Binding pKi = 6.4 6.4 -6 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1cccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)n1 10.1016/j.bmcl.2014.11.063
68028909 129358 None 0 Human Binding pKi = 6.4 6.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 553 9 1 5 4.7 CCCCc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670815 129358 None 0 Human Binding pKi = 6.4 6.4 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 553 9 1 5 4.7 CCCCc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
118721195 116089 None 0 Rat Binding pKi = 6.4 6.4 -9 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(C)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355945 116089 None 0 Rat Binding pKi = 6.4 6.4 -9 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(C)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44400977 69978 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 420 7 2 3 4.8 CC(C)CC(CNC(=O)Nc1ccc(Cl)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL193916 69978 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 420 7 2 3 4.8 CC(C)CC(CNC(=O)Nc1ccc(Cl)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44400944 70340 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 442 9 1 4 4.8 Cc1ccc(CCNCC(c2ccc(N(C)C)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL194435 70340 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 442 9 1 4 4.8 Cc1ccc(CCNCC(c2ccc(N(C)C)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
118721188 116081 None 0 Human Binding pKi = 6.4 6.4 2 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C(N)=O)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355937 116081 None 0 Human Binding pKi = 6.4 6.4 2 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 439 8 2 3 5.3 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C(N)=O)cc2)CC1 10.1016/j.bmcl.2014.11.063
44391312 65608 None 0 Human Binding pKi = 5.4 5.4 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 304 3 0 3 4.4 CCOc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL183229 65608 None 0 Human Binding pKi = 5.4 5.4 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 304 3 0 3 4.4 CCOc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
44389735 122390 None 0 Human Binding pKi = 6.3 6.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1cnc2ccccc2c1)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL359850 122390 None 0 Human Binding pKi = 6.3 6.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1cnc2ccccc2c1)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
118721195 116089 None 0 Human Binding pKi = 7.3 7.3 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(C)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355945 116089 None 0 Human Binding pKi = 7.3 7.3 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(C)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44389736 62856 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 513 5 0 3 6.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CF)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178422 62856 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 513 5 0 3 6.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CF)C2)CC1 10.1016/j.bmcl.2005.01.016
44389725 123722 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 482 4 0 4 5.5 O=C(c1cnnc2ccccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL362017 123722 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 482 4 0 4 5.5 O=C(c1cnnc2ccccc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
56966927 129337 None 0 Human Binding pKi = 7.3 7.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 456 6 1 5 3.6 COc1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670793 129337 None 0 Human Binding pKi = 7.3 7.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 456 6 1 5 3.6 COc1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
118721193 116087 None 0 Rat Binding pKi = 5.3 5.3 -69 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 398 7 2 3 5.2 OCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355943 116087 None 0 Rat Binding pKi = 5.3 5.3 -69 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 398 7 2 3 5.2 OCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
11952525 116102 None 0 Rat Binding pKi = 5.3 5.3 -38 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 562 10 0 5 8.0 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355958 116102 None 0 Rat Binding pKi = 5.3 5.3 -38 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 562 10 0 5 8.0 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)cc1 10.1016/j.bmcl.2014.11.063
44401129 126845 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 391 7 1 3 3.8 CN1CCN(C(CNCCc2ccccc2)c2ccc(C(F)(F)F)cc2)CC1 10.1021/jm040827u
CHEMBL365369 126845 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 391 7 1 3 3.8 CN1CCN(C(CNCCc2ccccc2)c2ccc(C(F)(F)F)cc2)CC1 10.1021/jm040827u
44401175 127298 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.5 COc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL365806 127298 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.5 COc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401037 71104 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 6 2 3 5.5 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1ccccc1 10.1021/jm040827u
CHEMBL195291 71104 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 6 2 3 5.5 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1ccccc1 10.1021/jm040827u
118721195 116089 None 0 Mouse Binding pKi = 7.3 7.3 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(C)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355945 116089 None 0 Mouse Binding pKi = 7.3 7.3 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(C)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44389765 169439 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4nccnc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL441848 169439 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4nccnc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
118721192 116085 None 0 Human Binding pKi = 6.3 6.3 -4 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 458 8 1 4 6.0 CCOC(=O)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355941 116085 None 0 Human Binding pKi = 6.3 6.3 -4 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 458 8 1 4 6.0 CCOC(=O)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44401146 70285 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 8 1 3 5.5 FC(F)(F)c1ccc(C(CNCCc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194135 70285 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 8 1 3 5.5 FC(F)(F)c1ccc(C(CNCCc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401256 71258 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 471 9 1 4 5.7 COc1ccccc1CCNCC(c1ccc(C(C)(C)C)cc1)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
CHEMBL195657 71258 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 471 9 1 4 5.7 COc1ccccc1CCNCC(c1ccc(C(C)(C)C)cc1)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
25024650 116104 None 0 Human Binding pKi = 8.3 8.3 21 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2014.11.063
CHEMBL3355960 116104 None 0 Human Binding pKi = 8.3 8.3 21 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cccc(C(=O)O)n1 10.1016/j.bmcl.2014.11.063
118721202 116106 None 0 Human Binding pKi = 8.3 8.3 15 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cc(C(=O)O)ccn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355962 116106 None 0 Human Binding pKi = 8.3 8.3 15 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cc(C(=O)O)ccn1 10.1016/j.bmcl.2014.11.063
9914506 81288 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 515 8 1 5 5.1 N#Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158769 81288 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 515 8 1 5 5.1 N#Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
68938028 81291 None 0 Human Binding pKi = 8.3 8.3 6 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158772 81291 None 0 Human Binding pKi = 8.3 8.3 6 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 8 1 4 5.6 Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
66615705 81298 None 0 Human Binding pKi = 8.3 8.3 19 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158779 81298 None 0 Human Binding pKi = 8.3 8.3 19 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2012.08.103
69826668 82272 None 0 Human Binding pKi = 8.3 8.3 5 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 524 5 0 5 4.9 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)c4cccc(S(C)(=O)=O)c4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171021 82272 None 0 Human Binding pKi = 8.3 8.3 5 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 524 5 0 5 4.9 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)c4cccc(S(C)(=O)=O)c4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
71457010 82290 None 0 Human Binding pKi = 8.3 8.3 10 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccccc1Cl)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171039 82290 None 0 Human Binding pKi = 8.3 8.3 10 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccccc1Cl)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
70790202 129352 None 0 Human Binding pKi = 8.3 8.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 553 8 1 5 4.8 CCC(C)N(C)C(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670809 129352 None 0 Human Binding pKi = 8.3 8.3 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 553 8 1 5 4.8 CCC(C)N(C)C(=O)c1cc(C)nc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
57718837 116076 None 0 Human Binding pKi = 8.2 8.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 414 7 1 2 6.4 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355932 116076 None 0 Human Binding pKi = 8.2 8.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 414 7 1 2 6.4 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
56966997 129355 None 0 Human Binding pKi = 8.2 8.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 555 6 1 5 3.8 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Br)c(C)c3)CC2)n1 nan
CHEMBL3670812 129355 None 0 Human Binding pKi = 8.2 8.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 555 6 1 5 3.8 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Br)c(C)c3)CC2)n1 nan
11466397 62899 None 0 Human Binding pKi = 7.3 7.3 -1 4
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178447 62899 None 0 Human Binding pKi = 7.3 7.3 -1 4
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
10003872 70306 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 449 9 1 4 5.1 COc1ccc(C(CNCCc2cc(C)cc(C)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194283 70306 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 449 9 1 4 5.1 COc1ccc(C(CNCCc2cc(C)cc(C)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
71451390 81297 None 0 Human Binding pKi = 7.3 7.3 7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 474 8 1 4 4.7 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158778 81297 None 0 Human Binding pKi = 7.3 7.3 7 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 474 8 1 4 4.7 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2012.08.103
22397436 82269 None 0 Human Binding pKi = 7.3 7.3 -6 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 510 5 0 5 4.5 CS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171019 82269 None 0 Human Binding pKi = 7.3 7.3 -6 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 510 5 0 5 4.5 CS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
17963258 82288 None 0 Human Binding pKi = 7.3 7.3 -2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 554 6 1 6 4.5 CN(C)c1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171037 82288 None 0 Human Binding pKi = 7.3 7.3 -2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 554 6 1 6 4.5 CN(C)c1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
71451671 82279 None 0 Human Binding pKi = 6.3 6.3 -31 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 519 8 2 5 5.0 O=C(O)CCNc1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171028 82279 None 0 Human Binding pKi = 6.3 6.3 -31 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 519 8 2 5 5.0 O=C(O)CCNc1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71451670 82267 None 0 Human Binding pKi = 5.3 5.3 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 455 7 1 4 4.2 COc1ccc(C(=O)NCCN2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)cc1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171017 82267 None 0 Human Binding pKi = 5.3 5.3 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 455 7 1 4 4.2 COc1ccc(C(=O)NCCN2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)cc1Cl 10.1016/j.bmcl.2012.08.124
44389751 64665 None 0 Human Binding pKi = 6.3 6.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 442 5 0 2 5.3 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(F)cc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL181794 64665 None 0 Human Binding pKi = 6.3 6.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 442 5 0 2 5.3 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(F)cc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
44401136 70800 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 495 9 1 3 6.8 Cc1cc(C)cc(CCNCC(c2ccc(-c3ccccc3)cc2)N2CCN(C3CCCCC3)CC2)c1 10.1021/jm040827u
CHEMBL195081 70800 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 495 9 1 3 6.8 Cc1cc(C)cc(CCNCC(c2ccc(-c3ccccc3)cc2)N2CCN(C3CCCCC3)CC2)c1 10.1021/jm040827u
44401132 68658 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 5 2 3 5.1 CN1CCN(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C(F)(F)F)cc2)CC1 10.1021/jm040827u
CHEMBL191824 68658 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 474 5 2 3 5.1 CN1CCN(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C(F)(F)F)cc2)CC1 10.1021/jm040827u
118721191 116084 None 0 Mouse Binding pKi = 7.3 7.3 -12 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 444 8 1 3 6.5 COC(C)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355940 116084 None 0 Mouse Binding pKi = 7.3 7.3 -12 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 444 8 1 3 6.5 COC(C)c1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
25024849 116103 None 0 Rat Binding pKi = 5.3 5.3 -97 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)nc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355959 116103 None 0 Rat Binding pKi = 5.3 5.3 -97 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)nc1 10.1016/j.bmcl.2014.11.063
44401012 68692 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 454 7 2 4 4.6 COc1ccccc1C(CNC(=O)Nc1ccc(F)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL192066 68692 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 454 7 2 4 4.6 COc1ccccc1C(CNC(=O)Nc1ccc(F)cc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44401145 70261 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 420 6 2 3 4.8 Cc1ccc(NC(=O)NCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194086 70261 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 420 6 2 3 4.8 Cc1ccc(NC(=O)NCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
25024849 116103 None 0 Human Binding pKi = 7.3 7.3 13 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)nc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355959 116103 None 0 Human Binding pKi = 7.3 7.3 13 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)nc1 10.1016/j.bmcl.2014.11.063
44401048 69871 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 473 8 1 3 5.8 Cc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193828 69871 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 473 8 1 3 5.8 Cc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
11952526 116097 None 0 Rat Binding pKi = 5.3 5.3 -1122 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 534 9 1 4 7.5 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355953 116097 None 0 Rat Binding pKi = 5.3 5.3 -1122 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 534 9 1 4 7.5 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
44401209 69826 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 418 6 2 3 4.5 O=C(NCC(c1ccccc1)N1CCN(c2ccccc2)CC1)Nc1ccc(F)cc1 10.1021/jm040827u
CHEMBL193592 69826 None 0 Human Binding pKi = 5.3 5.3 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 418 6 2 3 4.5 O=C(NCC(c1ccccc1)N1CCN(c2ccccc2)CC1)Nc1ccc(F)cc1 10.1021/jm040827u
44389683 131718 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL369287 131718 None 0 Human Binding pKi = 7.3 7.3 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2005.01.016
118721196 116090 None 0 Rat Binding pKi = 6.3 6.3 -6 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355946 116090 None 0 Rat Binding pKi = 6.3 6.3 -6 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
24937215 116096 None 0 Rat Binding pKi = 6.3 6.3 -9 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 472 9 1 4 5.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1CC(=O)O 10.1016/j.bmcl.2014.11.063
CHEMBL3355952 116096 None 0 Rat Binding pKi = 6.3 6.3 -9 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 472 9 1 4 5.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1CC(=O)O 10.1016/j.bmcl.2014.11.063
44401226 71131 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 429 9 1 4 4.7 COc1ccc(C(CNCCc2ccc(C)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL195406 71131 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 429 9 1 4 4.7 COc1ccc(C(CNCCc2ccc(C)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
56966929 129343 None 0 Human Binding pKi = 8.2 8.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 553 6 1 6 3.4 Cc1cc(C(=O)N2CCOCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670799 129343 None 0 Human Binding pKi = 8.2 8.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 553 6 1 6 3.4 Cc1cc(C(=O)N2CCOCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
11753159 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.103
7679 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158814 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.103
11753159 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
7679 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2158814 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
17963183 82294 None 0 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1cccc(Cl)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171043 82294 None 0 Human Binding pKi = 8.2 8.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1cccc(Cl)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
59296024 84043 None 0 Human Binding pKi = 8.2 8.2 9 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3ccc(S(C)(=O)=O)cc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207277 84043 None 0 Human Binding pKi = 8.2 8.2 9 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3ccc(S(C)(=O)=O)cc23)CC1 10.1016/j.bmcl.2012.09.112
59296111 84121 None 0 Human Binding pKi = 8.2 8.2 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 480 7 3 5 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
CHEMBL2207658 84121 None 0 Human Binding pKi = 8.2 8.2 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 480 7 3 5 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
56966995 129348 None 0 Human Binding pKi = 8.2 8.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 523 6 1 5 3.8 Cc1cc(C(=O)N2CCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670805 129348 None 0 Human Binding pKi = 8.2 8.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 523 6 1 5 3.8 Cc1cc(C(=O)N2CCC2)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
118721184 116077 None 0 Human Binding pKi = 7.2 7.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccccc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355933 116077 None 0 Human Binding pKi = 7.2 7.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccccc2)CC1 10.1016/j.bmcl.2014.11.063
25024850 116105 None 0 Human Binding pKi = 7.2 7.2 6 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1cccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)n1 10.1016/j.bmcl.2014.11.063
CHEMBL3355961 116105 None 0 Human Binding pKi = 7.2 7.2 6 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1cccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)n1 10.1016/j.bmcl.2014.11.063
44401005 70595 None 0 Human Binding pKi = 5.2 5.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 9 1 5 3.9 COc1ccccc1CC(=O)NCC(c1ccccc1OC)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
CHEMBL194886 70595 None 0 Human Binding pKi = 5.2 5.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 9 1 5 3.9 COc1ccccc1CC(=O)NCC(c1ccccc1OC)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
44401025 69699 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 496 9 1 4 5.5 CN(C)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL193535 69699 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 496 9 1 4 5.5 CN(C)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
11466397 62899 None 0 Mouse Binding pKi = 6.2 6.2 -83 4
In vitro binding affinity against mouse CC chemokine receptor 3In vitro binding affinity against mouse CC chemokine receptor 3
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178447 62899 None 0 Mouse Binding pKi = 6.2 6.2 -83 4
In vitro binding affinity against mouse CC chemokine receptor 3In vitro binding affinity against mouse CC chemokine receptor 3
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
24937215 116096 None 0 Human Binding pKi = 7.2 7.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 472 9 1 4 5.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1CC(=O)O 10.1016/j.bmcl.2014.11.063
CHEMBL3355952 116096 None 0 Human Binding pKi = 7.2 7.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 472 9 1 4 5.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1CC(=O)O 10.1016/j.bmcl.2014.11.063
70790203 129366 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 6 1 5 4.0 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3cc(C)c(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670823 129366 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 6 1 5 4.0 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3cc(C)c(Cl)c(C)c3)CC2)n1 nan
44391235 65266 None 0 Human Binding pKi = 5.2 5.2 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 376 1 0 4 4.1 N#C/N=c1/c2ccccc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL182719 65266 None 0 Human Binding pKi = 5.2 5.2 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 376 1 0 4 4.1 N#C/N=c1/c2ccccc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
118721185 116078 None 0 Mouse Binding pKi = 7.2 7.2 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355934 116078 None 0 Mouse Binding pKi = 7.2 7.2 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C)cc2)CC1 10.1016/j.bmcl.2014.11.063
25056323 71260 None 0 Human Binding pKi = 7.2 7.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.8 COc1ccc(C(CNCCc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL195671 71260 None 0 Human Binding pKi = 7.2 7.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.8 COc1ccc(C(CNCCc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401069 69132 None 0 Human Binding pKi = 4.2 4.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 473 7 1 3 5.3 O=C(Cc1cc(Cl)cc(Cl)c1)NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL192384 69132 None 0 Human Binding pKi = 4.2 4.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 473 7 1 3 5.3 O=C(Cc1cc(Cl)cc(Cl)c1)NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44401110 68676 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 9 1 4 5.8 COc1ccc(C(CNCCc2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL191959 68676 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 9 1 4 5.8 COc1ccc(C(CNCCc2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
59296041 84134 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 558 8 3 8 2.1 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(C#N)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207670 84134 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 558 8 3 8 2.1 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(C#N)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
25024651 116100 None 0 Mouse Binding pKi = 6.2 6.2 -39 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355956 116100 None 0 Mouse Binding pKi = 6.2 6.2 -39 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(C(=O)O)cn1 10.1016/j.bmcl.2014.11.063
118721185 116078 None 0 Rat Binding pKi = 6.2 6.2 -19 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355934 116078 None 0 Rat Binding pKi = 6.2 6.2 -19 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 410 7 1 2 6.5 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(C)cc2)CC1 10.1016/j.bmcl.2014.11.063
69347707 81336 None 0 Human Binding pKi = 6.2 6.2 -5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158833 81336 None 0 Human Binding pKi = 6.2 6.2 -5 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
69260079 81337 None 0 Human Binding pKi = 6.2 6.2 -63 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 463 6 1 5 4.8 O=C(O)c1cccnc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158834 81337 None 0 Human Binding pKi = 6.2 6.2 -63 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 463 6 1 5 4.8 O=C(O)c1cccnc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71457009 82281 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 5 1 4 5.2 Cc1ccc(C(=O)N2CCC(N3CC[C@H](Oc4ccc(Cl)c(C)c4Cl)C[C@@H]3C(=O)O)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171030 82281 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 504 5 1 4 5.2 Cc1ccc(C(=O)N2CCC(N3CC[C@H](Oc4ccc(Cl)c(C)c4Cl)C[C@@H]3C(=O)O)CC2)cc1 10.1016/j.bmcl.2012.08.124
17963199 82302 None 0 Human Binding pKi = 6.2 6.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 493 5 1 5 3.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(F)c(F)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171050 82302 None 0 Human Binding pKi = 6.2 6.2 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 493 5 1 5 3.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(F)c(F)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
44401203 70154 None 0 Human Binding pKi = 5.2 5.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 424 6 2 3 4.6 O=C(NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(F)cc1 10.1021/jm040827u
CHEMBL194026 70154 None 0 Human Binding pKi = 5.2 5.2 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 424 6 2 3 4.6 O=C(NCC(c1ccccc1)N1CCN(C2CCCCC2)CC1)Nc1ccc(F)cc1 10.1021/jm040827u
118721204 116108 None 0 Mouse Binding pKi = 7.2 7.2 -5 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 532 9 3 2 6.7 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)[nH]c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355964 116108 None 0 Mouse Binding pKi = 7.2 7.2 -5 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 532 9 3 2 6.7 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)[nH]c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
25024850 116105 None 0 Rat Binding pKi = 5.2 5.2 -107 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1cccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)n1 10.1016/j.bmcl.2014.11.063
CHEMBL3355961 116105 None 0 Rat Binding pKi = 5.2 5.2 -107 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1cccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)n1 10.1016/j.bmcl.2014.11.063
118721184 116077 None 0 Mouse Binding pKi = 7.2 7.2 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccccc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355933 116077 None 0 Mouse Binding pKi = 7.2 7.2 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccccc2)CC1 10.1016/j.bmcl.2014.11.063
11952524 116095 None 0 Mouse Binding pKi = 6.2 6.2 -9 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 490 8 0 3 7.8 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccccc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355951 116095 None 0 Mouse Binding pKi = 6.2 6.2 -9 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 490 8 0 3 7.8 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccccc1 10.1016/j.bmcl.2014.11.063
118721193 116087 None 0 Human Binding pKi = 7.2 7.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 398 7 2 3 5.2 OCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355943 116087 None 0 Human Binding pKi = 7.2 7.2 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 398 7 2 3 5.2 OCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44389684 63002 None 0 Human Binding pKi = 7.2 7.2 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 468 5 0 2 5.2 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178576 63002 None 0 Human Binding pKi = 7.2 7.2 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 468 5 0 2 5.2 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2005.01.016
118721206 116110 None 0 Mouse Binding pKi = 6.2 6.2 -19 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 667 11 2 6 7.3 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)OC)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355966 116110 None 0 Mouse Binding pKi = 6.2 6.2 -19 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 667 11 2 6 7.3 CCNC(=O)N[C@@H](CCN1CCC(c2c(CC)n(-c3ccc(C(=O)OC)cn3)c3cc(F)ccc23)CC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.11.063
11952524 116095 None 0 Human Binding pKi = 7.2 7.2 3 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 490 8 0 3 7.8 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccccc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355951 116095 None 0 Human Binding pKi = 7.2 7.2 3 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 490 8 0 3 7.8 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccccc1 10.1016/j.bmcl.2014.11.063
56966928 129338 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 440 5 1 4 3.9 Cc1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
CHEMBL3670794 129338 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 440 5 1 4 3.9 Cc1ccnc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)c1 nan
44389677 63108 None 0 Human Binding pKi = 7.2 7.2 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1cccc2cccnc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178875 63108 None 0 Human Binding pKi = 7.2 7.2 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 481 4 0 3 6.1 O=C(c1cccc2cccnc12)N1CCC(N2CCC(Cc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
56965997 129336 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 440 5 1 4 3.9 Cc1cccc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670792 129336 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 440 5 1 4 3.9 Cc1cccc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
118721201 116099 None 0 Human Binding pKi = 5.2 5.2 -2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 548 10 1 4 7.6 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355955 116099 None 0 Human Binding pKi = 5.2 5.2 -2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 548 10 1 4 7.6 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2014.11.063
11466397 62899 None 0 Rhesus macaque Binding pKi = 8.1 8.1 1 4
In vitro binding affinity against monkey CC chemokine receptor 3In vitro binding affinity against monkey CC chemokine receptor 3
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL178447 62899 None 0 Rhesus macaque Binding pKi = 8.1 8.1 1 4
In vitro binding affinity against monkey CC chemokine receptor 3In vitro binding affinity against monkey CC chemokine receptor 3
ChEMBL 511 5 1 4 5.3 O=C(c1ccc2ncccc2c1)N1CCC(N2CC[C@H](Cc3ccc(Cl)c(Cl)c3)[C@H](CO)C2)CC1 10.1016/j.bmcl.2005.01.016
11477767 63047 None 0 Human Binding pKi = 8.1 8.1 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL178818 63047 None 0 Human Binding pKi = 8.1 8.1 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 511 5 0 4 5.7 CO[C@@H]1CN(C2CCN(C(=O)c3ccc4ncccc4c3)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
67115945 129364 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 7 1 5 3.9 CCc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)cc(C)n3)CC2)ccc1Cl nan
CHEMBL3670821 129364 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 7 1 5 3.9 CCc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)cc(C)n3)CC2)ccc1Cl nan
56967065 129365 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 521 6 1 5 3.3 C#Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670822 129365 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 521 6 1 5 3.3 C#Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
71072052 81290 None 0 Human Binding pKi = 8.1 8.1 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 515 8 1 5 5.1 N#Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158771 81290 None 0 Human Binding pKi = 8.1 8.1 1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 515 8 1 5 5.1 N#Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
71453204 81301 None 0 Human Binding pKi = 8.1 8.1 12 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 488 8 1 4 5.0 Cc1cc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158782 81301 None 0 Human Binding pKi = 8.1 8.1 12 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 488 8 1 4 5.0 Cc1cc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
17963363 82286 None 0 Human Binding pKi = 8.1 8.1 2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccc(Cl)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171035 82286 None 0 Human Binding pKi = 8.1 8.1 2 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccc(Cl)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963226 82299 None 0 Human Binding pKi = 8.1 8.1 3 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 505 5 1 5 4.4 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4C)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171048 82299 None 0 Human Binding pKi = 8.1 8.1 3 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 505 5 1 5 4.4 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4C)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
59295994 84251 None 0 Human Binding pKi = 8.1 8.1 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cc(=O)[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208434 84251 None 0 Human Binding pKi = 8.1 8.1 -1 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cc(=O)[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
59295925 84135 None 0 Human Binding pKi = 8.1 8.1 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 567 8 3 7 2.9 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207671 84135 None 0 Human Binding pKi = 8.1 8.1 2 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation countingDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4-(methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting
ChEMBL 567 8 3 7 2.9 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
56966999 129361 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 495 6 1 5 3.1 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(F)c(C)c3)CC2)n1 nan
CHEMBL3670818 129361 None 0 Human Binding pKi = 7.2 7.2 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 495 6 1 5 3.1 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(F)c(C)c3)CC2)n1 nan
118721200 116098 None 0 Mouse Binding pKi = 7.1 7.1 -15 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 558 9 1 6 7.0 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(-c2nnn[nH]2)cc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355954 116098 None 0 Mouse Binding pKi = 7.1 7.1 -15 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 558 9 1 6 7.0 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1ccc(-c2nnn[nH]2)cc1 10.1016/j.bmcl.2014.11.063
67115364 124504 None 0 Human Binding pKi = 7.1 7.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 483 6 2 5 3.0 CNC(=O)c1cccc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3639696 124504 None 0 Human Binding pKi = 7.1 7.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 483 6 2 5 3.0 CNC(=O)c1cccc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
44391319 64359 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.3 Clc1ccc(/C=C2\CCN3Cc4ccccc4N=C23)cc1Cl 10.1016/j.bmcl.2004.11.039
CHEMBL181195 64359 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 328 1 0 2 5.3 Clc1ccc(/C=C2\CCN3Cc4ccccc4N=C23)cc1Cl 10.1016/j.bmcl.2004.11.039
118721190 116083 None 0 Rat Binding pKi = 6.1 6.1 -40 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 416 7 2 3 5.3 OCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355939 116083 None 0 Rat Binding pKi = 6.1 6.1 -40 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 416 7 2 3 5.3 OCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
24937215 116096 None 0 Mouse Binding pKi = 7.1 7.1 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 472 9 1 4 5.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1CC(=O)O 10.1016/j.bmcl.2014.11.063
CHEMBL3355952 116096 None 0 Mouse Binding pKi = 7.1 7.1 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 472 9 1 4 5.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1CC(=O)O 10.1016/j.bmcl.2014.11.063
25024849 116103 None 0 Mouse Binding pKi = 6.1 6.1 -13 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)nc1 10.1016/j.bmcl.2014.11.063
CHEMBL3355959 116103 None 0 Mouse Binding pKi = 6.1 6.1 -13 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)nc1 10.1016/j.bmcl.2014.11.063
44391170 65740 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 399 1 1 3 4.1 N=c1c2ccccc2nc2n1CC/C2=C\c1ccccc1I 10.1016/j.bmcl.2004.11.039
CHEMBL183461 65740 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 399 1 1 3 4.1 N=c1c2ccccc2nc2n1CC/C2=C\c1ccccc1I 10.1016/j.bmcl.2004.11.039
44400991 69835 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 471 9 1 4 5.7 COc1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL193633 69835 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 471 9 1 4 5.7 COc1ccc(CCNCC(c2ccc(C(C)(C)C)cc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
43957010 68659 None 9 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 399 6 2 4 3.0 CN1CCN(C(CNC(=O)Nc2ccc(F)cc2)c2ccc(N(C)C)cc2)CC1 10.1021/jm040827u
CHEMBL191828 68659 None 9 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 399 6 2 4 3.0 CN1CCN(C(CNC(=O)Nc2ccc(F)cc2)c2ccc(N(C)C)cc2)CC1 10.1021/jm040827u
118721186 116079 None 0 Human Binding pKi = 7.1 7.1 2 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(O)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355935 116079 None 0 Human Binding pKi = 7.1 7.1 2 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(O)cc2)CC1 10.1016/j.bmcl.2014.11.063
44401085 135574 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 527 8 1 3 6.5 FC(F)(F)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL372858 135574 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 527 8 1 3 6.5 FC(F)(F)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721202 116106 None 0 Mouse Binding pKi = 7.1 7.1 -15 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cc(C(=O)O)ccn1 10.1016/j.bmcl.2014.11.063
CHEMBL3355962 116106 None 0 Mouse Binding pKi = 7.1 7.1 -15 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 535 9 1 5 6.9 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1-c1cc(C(=O)O)ccn1 10.1016/j.bmcl.2014.11.063
68846936 81318 None 0 Human Binding pKi = 7.1 7.1 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
CHEMBL2158816 81318 None 0 Human Binding pKi = 7.1 7.1 -1 2
Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
23102733 82265 None 0 Human Binding pKi = 7.1 7.1 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 511 6 1 5 4.0 O=C(NS(=O)(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1)c1ccccc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171015 82265 None 0 Human Binding pKi = 7.1 7.1 1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 511 6 1 5 4.0 O=C(NS(=O)(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1)c1ccccc1 10.1016/j.bmcl.2012.08.124
71449858 82278 None 0 Human Binding pKi = 7.1 7.1 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 582 9 1 6 4.8 O=C(O)CCCS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171027 82278 None 0 Human Binding pKi = 7.1 7.1 -1 2
Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assayBinding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay
ChEMBL 582 9 1 6 4.8 O=C(O)CCCS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
71461541 84254 None 0 Human Binding pKi = 7.1 7.1 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 513 9 3 6 2.7 CS(=O)(=O)c1ccccc1C(=O)NCC(O)CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208437 84254 None 0 Human Binding pKi = 7.1 7.1 15 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 513 9 3 6 2.7 CS(=O)(=O)c1ccccc1C(=O)NCC(O)CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
44391240 123725 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 432 2 0 2 6.7 Fc1ccc(C2C/C(=C\c3ccccc3Br)C3=Nc4ccccc4CN32)cc1 10.1016/j.bmcl.2004.11.039
CHEMBL362032 123725 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 432 2 0 2 6.7 Fc1ccc(C2C/C(=C\c3ccccc3Br)C3=Nc4ccccc4CN32)cc1 10.1016/j.bmcl.2004.11.039
44389732 64369 None 0 Human Binding pKi = 6.1 6.1 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 420 6 0 3 4.5 COc1ccc(CC2CCN(C3CCN(C(=O)Cc4ccccc4C)CC3)CC2)cc1 10.1016/j.bmcl.2005.01.016
CHEMBL181230 64369 None 0 Human Binding pKi = 6.1 6.1 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 420 6 0 3 4.5 COc1ccc(CC2CCN(C3CCN(C(=O)Cc4ccccc4C)CC3)CC2)cc1 10.1016/j.bmcl.2005.01.016
71450777 84237 None 0 Human Binding pKi = 6.1 6.1 -63 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 404 7 0 4 5.2 N#Cc1cccc(OCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208420 84237 None 0 Human Binding pKi = 6.1 6.1 -63 2
Displacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-4-(2,4-dichloro-3-methylphenoxy)-l'-[4- (methylsulfonyl)benzoyl]-l,4'-bipiperidine from human recombinant CCR3 expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 404 7 0 4 5.2 N#Cc1cccc(OCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
56965994 129356 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 7 1 5 3.9 CCc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
CHEMBL3670813 129356 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 525 7 1 5 3.9 CCc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C)c3)CC2)n1 nan
56965996 129341 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 497 6 1 5 3.3 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)ccn3)CC2)ccc1Cl nan
CHEMBL3670797 129341 None 0 Human Binding pKi = 8.1 8.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 497 6 1 5 3.3 Cc1cc(CN2CCC(N3C(=O)CC[C@@H]3C(=O)Nc3cc(C(=O)N(C)C)ccn3)CC2)ccc1Cl nan
25056324 127013 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 8 1 3 5.8 Clc1cc(Cl)cc(CCNCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)c1 10.1021/jm040827u
CHEMBL365551 127013 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 459 8 1 3 5.8 Clc1cc(Cl)cc(CCNCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)c1 10.1021/jm040827u
44401070 69133 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 414 6 2 3 4.7 Cc1ccc(NC(=O)NCC(c2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
CHEMBL192385 69133 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 414 6 2 3 4.7 Cc1ccc(NC(=O)NCC(c2ccccc2)N2CCN(c3ccccc3)CC2)cc1 10.1021/jm040827u
24937092 116101 None 0 Human Binding pKi = 7.1 7.1 2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 500 10 0 5 6.4 CCOC(=O)Cn1c(CC)c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2014.11.063
CHEMBL3355957 116101 None 0 Human Binding pKi = 7.1 7.1 2 2
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 500 10 0 5 6.4 CCOC(=O)Cn1c(CC)c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2014.11.063
44391282 122687 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 352 1 1 4 3.6 N=c1c2cccnc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL360308 122687 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 352 1 1 4 3.6 N=c1c2cccnc2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
136216709 78997 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 341 1 2 4 2.9 N=c1c2nc[nH]c2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
CHEMBL2113024 78997 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 341 1 2 4 2.9 N=c1c2nc[nH]c2nc2n1CC/C2=C\c1ccccc1Br 10.1016/j.bmcl.2004.11.039
44387847 60515 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.8 COc1ccc(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL175547 60515 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.8 COc1ccc(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44387853 63465 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 515 8 1 3 6.8 CC(C)(C)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL179752 63465 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 515 8 1 3 6.8 CC(C)(C)c1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
57718829 116094 None 0 Mouse Binding pKi = 7.1 7.1 -2 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 428 7 0 3 6.4 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1C 10.1016/j.bmcl.2014.11.063
CHEMBL3355950 116094 None 0 Mouse Binding pKi = 7.1 7.1 -2 2
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 428 7 0 3 6.4 CCc1c(C2CCN(CCCSc3ccc(F)cc3)CC2)c2ccc(F)cc2n1C 10.1016/j.bmcl.2014.11.063
118721196 116090 None 0 Human Binding pKi = 7.1 7.1 4 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355946 116090 None 0 Human Binding pKi = 7.1 7.1 4 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 412 7 2 3 5.9 CCc1[nH]c2cc(O)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44389790 64793 None 0 Human Binding pKi = 7.1 7.1 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3cnnc4ccccc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
CHEMBL181929 64793 None 0 Human Binding pKi = 7.1 7.1 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 512 5 0 5 5.1 CO[C@@H]1CN(C2CCN(C(=O)c3cnnc4ccccc34)CC2)CC[C@@H]1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.01.016
56967063 129362 None 0 Human Binding pKi = 7.1 7.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 565 6 1 5 4.4 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C(F)(F)F)c3)CC2)n1 nan
CHEMBL3670819 129362 None 0 Human Binding pKi = 7.1 7.1 - 1
Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well.
ChEMBL 565 6 1 5 4.4 Cc1cc(C(=O)N(C)C)cc(NC(=O)[C@H]2CCC(=O)N2C2CCN(Cc3ccc(Cl)c(C(F)(F)F)c3)CC2)n1 nan
118721184 116077 None 0 Rat Binding pKi = 6.1 6.1 -14 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccccc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355933 116077 None 0 Rat Binding pKi = 6.1 6.1 -14 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 396 7 1 2 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccccc2)CC1 10.1016/j.bmcl.2014.11.063
44400974 135359 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 485 8 1 4 5.2 COc1ccccc1CC(=O)NCC(c1ccc(C(C)(C)C)cc1)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
CHEMBL372725 135359 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 485 8 1 4 5.2 COc1ccccc1CC(=O)NCC(c1ccc(C(C)(C)C)cc1)N1CCN(c2ccccc2)CC1 10.1021/jm040827u
44400949 69178 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 8 1 3 5.7 Fc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL192412 69178 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 477 8 1 3 5.7 Fc1ccc(CCNCC(c2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401155 70197 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.8 COc1ccccc1C(CNC(=O)Nc1cc(Cl)cc(Cl)c1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
CHEMBL194044 70197 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 504 7 2 4 5.8 COc1ccccc1C(CNC(=O)Nc1cc(Cl)cc(Cl)c1)N1CCN(C2CCCCC2)CC1 10.1021/jm040827u
44401094 71153 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 391 7 1 3 3.8 CN1CCN(C(CNCCc2ccc(C(F)(F)F)cc2)c2ccccc2)CC1 10.1021/jm040827u
CHEMBL195488 71153 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 391 7 1 3 3.8 CN1CCN(C(CNCCc2ccc(C(F)(F)F)cc2)c2ccccc2)CC1 10.1021/jm040827u
11397231 81494 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of CCR3 receptorInhibition of CCR3 receptor
ChEMBL 469 7 0 4 6.2 Fc1ccc(SCCCN2CCC(n3c(CC(F)(F)F)nc4cc(F)ccc43)CC2)cc1 10.1016/j.bmc.2012.09.013
CHEMBL2159766 81494 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of CCR3 receptorInhibition of CCR3 receptor
ChEMBL 469 7 0 4 6.2 Fc1ccc(SCCCN2CCC(n3c(CC(F)(F)F)nc4cc(F)ccc43)CC2)cc1 10.1016/j.bmc.2012.09.013
9797962 65695 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 338 1 0 2 4.8 Brc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
CHEMBL183429 65695 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 338 1 0 2 4.8 Brc1ccccc1/C=C1\CCN2Cc3ccccc3N=C12 10.1016/j.bmcl.2004.11.039
44401032 70152 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 492 7 2 4 5.8 COc1ccc(C(CNC(=O)Nc2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL194022 70152 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 492 7 2 4 5.8 COc1ccc(C(CNC(=O)Nc2ccc(C(C)(C)C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401234 69863 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 435 9 1 4 4.8 COc1ccc(C(CNCCc2ccc(C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL193809 69863 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 435 9 1 4 4.8 COc1ccc(C(CNCCc2ccc(C)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721193 116087 None 0 Mouse Binding pKi = 7.0 7.0 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 398 7 2 3 5.2 OCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355943 116087 None 0 Mouse Binding pKi = 7.0 7.0 -1 3
Displacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from mouse CCR3 transfected in CHO cells
ChEMBL 398 7 2 3 5.2 OCc1[nH]c2ccccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
44401089 124126 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.5 COc1ccc(C(CNCCc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL363181 124126 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 489 9 1 4 5.5 COc1ccc(C(CNCCc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44391268 63920 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 312 1 0 2 4.8 Fc1ccc(/C=C2\CCN3Cc4ccccc4N=C23)c(Cl)c1 10.1016/j.bmcl.2004.11.039
CHEMBL180493 63920 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membraneBinding affinity measured for human C-C chemokine receptor type 3 expressed on human K562 cell membrane
ChEMBL 312 1 0 2 4.8 Fc1ccc(/C=C2\CCN3Cc4ccccc4N=C23)c(Cl)c1 10.1016/j.bmcl.2004.11.039
44387857 61054 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 542 6 2 3 6.8 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm040827u
CHEMBL176281 61054 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 542 6 2 3 6.8 O=C(NCC(c1ccc(C(F)(F)F)cc1)N1CCN(C2CCCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm040827u
44389729 64370 None 0 Human Binding pKi = 6.0 6.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(Cl)cc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
CHEMBL181232 64370 None 0 Human Binding pKi = 6.0 6.0 - 1
In vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell lineIn vitro binding affinity against C-C chemokine receptor type 3 expressing in rat Y3 cell line
ChEMBL 458 5 0 2 5.8 Cc1ccccc1CC(=O)N1CCC(N2CCC(Cc3cc(Cl)cc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2005.01.016
118721187 116080 None 0 Rat Binding pKi = 6.0 6.0 -10 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(OC)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355936 116080 None 0 Rat Binding pKi = 6.0 6.0 -10 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(OC)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721187 116080 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(OC)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355936 116080 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 426 8 1 3 6.2 CCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(OC)cc2)CC1 10.1016/j.bmcl.2014.11.063
44400978 135953 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 530 6 2 3 6.8 CC(C)(C)c1ccc(C(CNC(=O)Nc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL373092 135953 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 530 6 2 3 6.8 CC(C)(C)c1ccc(C(CNC(=O)Nc2ccc(C(F)(F)F)cc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721203 116107 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccnc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355963 116107 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccnc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)c1 10.1016/j.bmcl.2014.11.063
44400983 71162 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 436 7 2 4 4.5 COc1ccc(NC(=O)NCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL195533 71162 None 0 Human Binding pKi = 5.0 5.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 436 7 2 4 4.5 COc1ccc(NC(=O)NCC(c2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
44401176 68423 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 517 7 2 4 5.9 CN(C)c1ccc(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
CHEMBL191696 68423 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)Inhibition of [125I]eotaxin-1 binding to human chemokine receptor (hCCR3-C1)
ChEMBL 517 7 2 4 5.9 CN(C)c1ccc(C(CNC(=O)Nc2cc(Cl)cc(Cl)c2)N2CCN(C3CCCCC3)CC2)cc1 10.1021/jm040827u
118721190 116083 None 0 Human Binding pKi = 7 7.0 -5 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 416 7 2 3 5.3 OCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
CHEMBL3355939 116083 None 0 Human Binding pKi = 7 7.0 -5 3
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cellsDisplacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
ChEMBL 416 7 2 3 5.3 OCc1[nH]c2cc(F)ccc2c1C1CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.11.063
118721203 116107 None 0 Rat Binding pKi = 6 6.0 -10 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccnc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)c1 10.1016/j.bmcl.2014.11.063
CHEMBL3355963 116107 None 0 Rat Binding pKi = 6 6.0 -10 3
Displacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cellsDisplacement of [125J]-eotaxin-1 from rat CCR3 transfected in CHO cells
ChEMBL 563 10 0 6 7.4 CCOC(=O)c1ccnc(-n2c(CC)c(C3CCN(CCCSc4ccc(F)cc4)CC3)c3ccc(F)cc32)c1 10.1016/j.bmcl.2014.11.063
795 574 None 5 Human Binding pKd None 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
796 574 None 5 Human Binding pKd None 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
9913085 574 None 5 Human Binding pKd None 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
CHEMBL20921 574 None 5 Human Binding pKd None 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
11753159 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Assay using sodium salt of the compoundAssay using sodium salt of the compound
Guide to Pharmacology 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 23031591
7679 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Assay using sodium salt of the compoundAssay using sodium salt of the compound
Guide to Pharmacology 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 23031591
CHEMBL2158814 547 None 6 Human Binding pKi = 8.2 8.2 1 2
Assay using sodium salt of the compoundAssay using sodium salt of the compound
Guide to Pharmacology 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 23031591
10653 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.
Guide to Pharmacology 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C None
59534386 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.
Guide to Pharmacology 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C None
CHEMBL3670800 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.
Guide to Pharmacology 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C None
DB15269 2288 None 15 Human Binding pKi = 8.5 8.5 - 1
Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.Dissociation constant determined in a scintillation proximity binding assay using recombinant human [<sup>125</sup>]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.
Guide to Pharmacology 511 6 1 5 3.6 O=C([C@H]1CCC(=O)N1C1CCN(CC1)Cc1ccc(c(c1)C)Cl)Nc1nc(C)cc(c1)C(=O)N(C)C None
3492 692 None 0 Human Binding pKi = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 12067561
9868459 692 None 0 Human Binding pKi = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 12067561
CHEMBL50593 692 None 0 Human Binding pKi = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 451 10 3 4 4.5 CC[C@@H]([C@H]1C[C@H](CCN1CCCNC(=O)Nc1cccc(c1)C(=O)C)Cc1ccccc1)O 12067561
3530 3518 None 0 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 378 6 1 5 3.3 COC(=O)[C@@H](NC(=O)c1ccc2c(c1)cccc2)Cc1ccc(cc1)N(=O)=O None
5311092 3518 None 0 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 378 6 1 5 3.3 COC(=O)[C@@H](NC(=O)c1ccc2c(c1)cccc2)Cc1ccc(cc1)N(=O)=O None
795 574 None 5 Human Binding pKi = 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
796 574 None 5 Human Binding pKi = 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
9913085 574 None 5 Human Binding pKi = 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
CHEMBL20921 574 None 5 Human Binding pKi = 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 12450563
758 865 None 0 Human Binding pKi = 8.9 8.9 -3 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8642344
759 866 None 0 Human Binding pKi = 8.9 8.9 6 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8642344
787 826 None 0 Human Binding pKi = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8642344
769 827 None 0 Human Binding pKi = 9.9 9.9 446 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8642344
771 838 None 0 Human Binding pKi None 7.5 7.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8642344