Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
14434082 90558 17 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccnc2c1ccc1c(C=O)ccnc12 10.1021/jm301121j
CHEMBL2205801 90558 17 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccnc2c1ccc1c(C=O)ccnc12 10.1021/jm301121j
14434082 90558 17 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccnc2c1ccc1c(C=O)ccnc12 10.1021/jm301121j
CHEMBL2205801 90558 17 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccnc2c1ccc1c(C=O)ccnc12 10.1021/jm301121j
72791 215019 76 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL98682 215019 76 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
72791 215019 76 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL98682 215019 76 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
77865 114063 82 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL317115 114063 82 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
14338 11140 124 None 3 3 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
CHEMBL101165 11140 124 None 3 3 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
77865 114063 82 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL317115 114063 82 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
14338 11140 124 None 3 3 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
CHEMBL101165 11140 124 None 3 3 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
667748 90561 86 None 3 3 Human 6.4 pEC50 = 6.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 267 2 0 3 3.9 Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 10.1021/jm301121j
CHEMBL2205805 90561 86 None 3 3 Human 6.4 pEC50 = 6.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 267 2 0 3 3.9 Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 10.1021/jm301121j
12425 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
1318 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
CHEMBL415879 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
DB02365 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
667748 90561 86 None 3 3 Human 6.4 pEC50 = 6.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 267 2 0 3 3.9 Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 10.1021/jm301121j
CHEMBL2205805 90561 86 None 3 3 Human 6.4 pEC50 = 6.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 267 2 0 3 3.9 Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 10.1021/jm301121j
12425 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
1318 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
CHEMBL415879 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
DB02365 6795 126 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
1474 161178 142 None -1 3 Human 4.4 pEC50 = 4.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
CHEMBL39879 161178 142 None -1 3 Human 4.4 pEC50 = 4.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
1474 161178 142 None -1 3 Human 4.4 pEC50 = 4.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
CHEMBL39879 161178 142 None -1 3 Human 4.4 pEC50 = 4.4 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
74265 215126 115 None 2 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 0 0 2 4.0 Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C 10.1021/jm301121j
CHEMBL99384 215126 115 None 2 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 0 0 2 4.0 Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C 10.1021/jm301121j
20445 90562 115 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1cccc(-c2cccc(C)n2)n1 10.1021/jm301121j
CHEMBL2205806 90562 115 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1cccc(-c2cccc(C)n2)n1 10.1021/jm301121j
70848 213451 112 None 5 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
CHEMBL89445 213451 112 None 5 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
72792 206502 84 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 206502 84 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
74265 215126 115 None 2 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 0 0 2 4.0 Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C 10.1021/jm301121j
CHEMBL99384 215126 115 None 2 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 0 0 2 4.0 Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C 10.1021/jm301121j
20445 90562 115 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1cccc(-c2cccc(C)n2)n1 10.1021/jm301121j
CHEMBL2205806 90562 115 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1cccc(-c2cccc(C)n2)n1 10.1021/jm301121j
2733927 90564 97 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
CHEMBL2205808 90564 97 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
70848 213451 112 None 5 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
CHEMBL89445 213451 112 None 5 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
72792 206502 84 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 206502 84 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
2733927 90564 97 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
CHEMBL2205808 90564 97 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
15783796 90567 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
CHEMBL2205810 90567 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
93149 113978 84 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
CHEMBL316589 113978 84 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
12987698 90565 4 None -3 3 Human 5.2 pEC50 = 5.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
CHEMBL2205809 90565 4 None -3 3 Human 5.2 pEC50 = 5.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
15783796 90567 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
CHEMBL2205810 90567 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
93149 113978 84 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
CHEMBL316589 113978 84 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
12987698 90565 4 None -3 3 Human 5.2 pEC50 = 5.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
CHEMBL2205809 90565 4 None -3 3 Human 5.2 pEC50 = 5.2 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
15664 90563 101 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
CHEMBL2205807 90563 101 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
15664 90563 101 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
CHEMBL2205807 90563 101 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
77524 62661 100 None - 1 Human 4.1 pEC50 = 4.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 212 0 2 4 2.2 Oc1ccnc2c1ccc1c(O)ccnc12 10.1021/jm301121j
CHEMBL1623498 62661 100 None - 1 Human 4.1 pEC50 = 4.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 212 0 2 4 2.2 Oc1ccnc2c1ccc1c(O)ccnc12 10.1021/jm301121j
77524 62661 100 None - 1 Human 4.1 pEC50 = 4.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 212 0 2 4 2.2 Oc1ccnc2c1ccc1c(O)ccnc12 10.1021/jm301121j
CHEMBL1623498 62661 100 None - 1 Human 4.1 pEC50 = 4.1 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 212 0 2 4 2.2 Oc1ccnc2c1ccc1c(O)ccnc12 10.1021/jm301121j
10391001 143976 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL374939 143976 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
11541506 83291 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 575 9 2 5 5.7 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)C1 10.1021/jm050965z
CHEMBL205993 83291 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 575 9 2 5 5.7 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)C1 10.1021/jm050965z
16105860 143981 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 507 8 2 4 4.7 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(CC)cc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL374978 143981 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 507 8 2 4 4.7 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(CC)cc3)c3ccccc23)CC1 10.1021/jm061118e
16105782 89480 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 482 6 2 6 3.4 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccncc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL217965 89480 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 482 6 2 6 3.4 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccncc3)c3ccccc23)CC1 10.1021/jm061118e
16112836 100140 2 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR8 expressed in Th2 cells assessed as I309 mediated migration by chemotaxis assayAntagonist activity at human recombinant CCR8 expressed in Th2 cells assessed as I309 mediated migration by chemotaxis assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc([C@@H]3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL245568 100140 2 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR8 expressed in Th2 cells assessed as I309 mediated migration by chemotaxis assayAntagonist activity at human recombinant CCR8 expressed in Th2 cells assessed as I309 mediated migration by chemotaxis assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc([C@@H]3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439843 98315 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 426 4 1 4 4.9 O=C1OC(c2ccnc3ccccc23)CN1C1CCN(Cc2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2006.12.076
CHEMBL240462 98315 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 426 4 1 4 4.9 O=C1OC(c2ccnc3ccccc23)CN1C1CCN(Cc2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2006.12.076
16105780 91376 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 481 7 2 6 3.0 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cnccn3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL222112 91376 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 481 7 2 6 3.0 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cnccn3)c3ccccc23)CC1 10.1021/jm061118e
44598057 203849 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 421 6 0 4 4.6 CC(C)COc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm900713y
CHEMBL567419 203849 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 421 6 0 4 4.6 CC(C)COc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm900713y
11533398 82761 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 499 8 2 5 4.9 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)CC2)c1 10.1021/jm050965z
CHEMBL205447 82761 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 499 8 2 5 4.9 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)CC2)c1 10.1021/jm050965z
44457090 104438 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 471 6 0 5 5.4 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm900713y
CHEMBL271128 104438 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 471 6 0 5 5.4 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm900713y
11950828 104397 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1cc[n+]([O-])cc1)CC2 10.1021/jm070543k
CHEMBL270971 104397 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1cc[n+]([O-])cc1)CC2 10.1021/jm070543k
11950828 104397 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1cc[n+]([O-])cc1)CC2 10.1021/jm900713y
CHEMBL270971 104397 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1cc[n+]([O-])cc1)CC2 10.1021/jm900713y
44457090 104438 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 471 6 0 5 5.4 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm070543k
CHEMBL271128 104438 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 471 6 0 5 5.4 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm070543k
44457009 165787 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 504 6 0 4 6.7 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccc(Cl)cc2)CC3)c1 10.1021/jm070543k
CHEMBL409648 165787 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 504 6 0 4 6.7 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccc(Cl)cc2)CC3)c1 10.1021/jm070543k
16105857 172981 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 479 7 2 4 4.2 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL426551 172981 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 479 7 2 4 4.2 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
10480554 156994 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 5 0 5 5.7 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(Cl)c(Cl)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL395211 156994 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 5 0 5 5.7 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(Cl)c(Cl)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439881 100575 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 457 5 0 6 5.1 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6o5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247563 100575 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 457 5 0 6 5.1 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6o5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
10004785 100619 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 467 5 0 5 5.6 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc6ccccc6c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247762 100619 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 467 5 0 5 5.6 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc6ccccc6c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439890 100690 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 447 6 0 6 4.4 COc1ccc(CN2CCC(N3CC(c4ccnc5ccc(OC)cc45)OC3=O)CC2)cc1 10.1016/j.bmcl.2006.12.076
CHEMBL248171 100690 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 447 6 0 6 4.4 COc1ccc(CN2CCC(N3CC(c4ccnc5ccc(OC)cc45)OC3=O)CC2)cc1 10.1016/j.bmcl.2006.12.076
44439886 100651 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 417 5 0 5 4.4 COc1ccc2nccc(C3CN(C4CCN(Cc5ccccc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247964 100651 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 417 5 0 5 4.4 COc1ccc2nccc(C3CN(C4CCN(Cc5ccccc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439895 157245 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 442 5 0 6 4.3 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(C#N)cc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL395423 157245 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 442 5 0 6 4.3 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(C#N)cc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
16065425 204007 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 405 3 0 4 3.9 CC1Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccncc3)CC4)c2O1 10.1021/jm900713y
CHEMBL568296 204007 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 405 3 0 4 3.9 CC1Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccncc3)CC4)c2O1 10.1021/jm900713y
16105885 89548 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 580 11 2 6 5.0 CCN(CC)CCCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL217984 89548 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 580 11 2 6 5.0 CCN(CC)CCCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
44598821 204717 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 472 6 0 6 4.8 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncn1)CC2 10.1021/jm900713y
CHEMBL573216 204717 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 472 6 0 6 4.8 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncn1)CC2 10.1021/jm900713y
44598059 203791 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 442 5 0 5 4.8 O=C(c1ccncn1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm900713y
CHEMBL566974 203791 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 442 5 0 5 4.8 O=C(c1ccncn1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm900713y
44598769 203878 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 422 6 0 5 4.0 CC(C)COc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncn1)CC2 10.1021/jm900713y
CHEMBL567620 203878 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 422 6 0 5 4.0 CC(C)COc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncn1)CC2 10.1021/jm900713y
16105854 90687 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 485 8 2 4 4.4 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)CC3CCCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL220650 90687 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 485 8 2 4 4.4 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)CC3CCCC3)c3ccccc23)CC1 10.1021/jm061118e
16065428 204637 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 391 3 0 4 3.5 O=C(c1ccncc1)N1CCC2(CCN(Cc3cccc4c3OCC4)CC2)CC1 10.1021/jm900713y
CHEMBL572537 204637 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 391 3 0 4 3.5 O=C(c1ccncc1)N1CCC2(CCN(Cc3cccc4c3OCC4)CC2)CC1 10.1021/jm900713y
16105774 91099 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 535 10 2 4 5.5 CCCCc1ccc(C(=O)Nc2ccc(S(=O)(=O)NC3CCN(C(=O)CCC)CC3)c3ccccc23)cc1 10.1021/jm061118e
CHEMBL221601 91099 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 535 10 2 4 5.5 CCCCc1ccc(C(=O)Nc2ccc(S(=O)(=O)NC3CCN(C(=O)CCC)CC3)c3ccccc23)cc1 10.1021/jm061118e
3384970 168060 8 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 432 6 2 4 4.9 COc1ccc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)cc1 10.1021/jm061118e
CHEMBL412116 168060 8 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 432 6 2 4 4.9 COc1ccc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)cc1 10.1021/jm061118e
16105862 90164 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 469 7 2 5 3.8 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccoc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL219432 90164 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 469 7 2 5 3.8 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccoc3)c3ccccc23)CC1 10.1021/jm061118e
44439837 154755 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 8 2 5 4.4 COc1ccc2nccc(C3CN(CCCNCc4cc5ccccc5[nH]4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL393411 154755 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 8 2 5 4.4 COc1ccc2nccc(C3CN(CCCNCc4cc5ccccc5[nH]4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44457089 104437 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 471 6 0 5 5.4 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccccn1)CC2 10.1021/jm070543k
CHEMBL271127 104437 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 471 6 0 5 5.4 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccccn1)CC2 10.1021/jm070543k
11950826 165968 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 457 5 0 4 4.6 O=C(c1cc[n+]([O-])cc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
CHEMBL409849 165968 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 457 5 0 4 4.6 O=C(c1cc[n+]([O-])cc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
44456993 104563 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 441 5 0 4 5.4 O=C(c1ccncc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm900713y
CHEMBL271801 104563 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 441 5 0 4 5.4 O=C(c1ccncc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm900713y
44456993 104563 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 441 5 0 4 5.4 O=C(c1ccncc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
CHEMBL271801 104563 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 441 5 0 4 5.4 O=C(c1ccncc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
44598060 204045 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 0 5 4.1 CC1(C)CCc2cc(CN3CCC4(CC3)CCN(C(=O)c3ccncn3)CC4)ccc2O1 10.1021/jm900713y
CHEMBL568503 204045 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 0 5 4.1 CC1(C)CCc2cc(CN3CCC4(CC3)CCN(C(=O)c3ccncn3)CC4)ccc2O1 10.1021/jm900713y
44457046 174114 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
CHEMBL429436 174114 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
44457046 174114 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm900713y
CHEMBL429436 174114 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm900713y
16105772 90148 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 497 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3F)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL219380 90148 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 497 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3F)c3ccccc23)CC1 10.1021/jm061118e
16105819 91265 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 622 9 2 7 4.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN3CC(C)OC(C)C3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL222020 91265 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 622 9 2 7 4.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN3CC(C)OC(C)C3)CC2)c2ccccc12 10.1021/jm061118e
16112836 100140 2 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc([C@@H]3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL245568 100140 2 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc([C@@H]3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
45483901 203848 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 476 6 1 5 5.1 CCCC1(CC)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2O1 10.1021/jm900713y
CHEMBL567417 203848 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 476 6 1 5 5.1 CCCC1(CC)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2O1 10.1021/jm900713y
16064872 204050 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)c2O1 10.1021/jm900713y
CHEMBL568523 204050 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)c2O1 10.1021/jm900713y
44598124 205417 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 470 3 1 5 4.4 CC1(C)Oc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2C1(F)F 10.1021/jm900713y
CHEMBL579072 205417 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 470 3 1 5 4.4 CC1(C)Oc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2C1(F)F 10.1021/jm900713y
45483880 204006 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 476 3 1 5 4.9 CC(C)(C)C1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2O1 10.1021/jm900713y
CHEMBL568294 204006 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 476 3 1 5 4.9 CC(C)(C)C1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2O1 10.1021/jm900713y
16105859 91104 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 497 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccc(F)c3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221639 91104 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 497 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccc(F)c3)c3ccccc23)CC1 10.1021/jm061118e
16105864 91139 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 483 7 2 6 2.9 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3nccn3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221842 91139 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 483 7 2 6 2.9 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3nccn3C)c3ccccc23)CC1 10.1021/jm061118e
16105855 89918 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 487 7 2 5 3.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCOCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218209 89918 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 487 7 2 5 3.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCOCC3)c3ccccc23)CC1 10.1021/jm061118e
11584004 147476 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 489 7 2 4 5.1 O=C(NC1CCN(Cc2cccc(Oc3ccccc3Cl)c2)CC1)C1(c2ccccc2)CCNC1 10.1021/jm050965z
CHEMBL381619 147476 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 489 7 2 4 5.1 O=C(NC1CCN(Cc2cccc(Oc3ccccc3Cl)c2)CC1)C1(c2ccccc2)CCNC1 10.1021/jm050965z
45483913 203708 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ncccc3N)CC4)c2O1 10.1021/jm900713y
CHEMBL566324 203708 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ncccc3N)CC4)c2O1 10.1021/jm900713y
44598121 203879 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccnc(N)c3)CC4)cccc2O1 10.1021/jm900713y
CHEMBL567627 203879 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccnc(N)c3)CC4)cccc2O1 10.1021/jm900713y
16105777 143737 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 535 7 2 5 5.4 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc4ccccc4s3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL374414 143737 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 535 7 2 5 5.4 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc4ccccc4s3)c3ccccc23)CC1 10.1021/jm061118e
16105776 143713 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 585 10 2 5 5.7 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(OCc4ccccc4)cc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL374274 143713 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 585 10 2 5 5.7 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(OCc4ccccc4)cc3)c3ccccc23)CC1 10.1021/jm061118e
9911916 98454 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL240848 98454 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
10433657 100652 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 445 7 0 5 4.8 COc1ccc2nccc(C3CN(C4CCN(CCCc5ccccc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247965 100652 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 445 7 0 5 4.8 COc1ccc2nccc(C3CN(C4CCN(CCCc5ccccc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
11842667 167825 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2cccc[n+]2[O-])CC3)c1 10.1021/jm070543k
CHEMBL411651 167825 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2cccc[n+]2[O-])CC3)c1 10.1021/jm070543k
44456948 166896 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 442 5 0 5 4.8 O=C(c1ccncn1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
CHEMBL410885 166896 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 442 5 0 5 4.8 O=C(c1ccncn1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm070543k
44456948 166896 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 442 5 0 5 4.8 O=C(c1ccncn1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm900713y
CHEMBL410885 166896 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 442 5 0 5 4.8 O=C(c1ccncn1)N1CCC2(CCN(Cc3cccc(Oc4ccccc4)c3)CC2)CC1 10.1021/jm900713y
16105887 91122 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 640 9 2 6 5.7 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN3CCc4ccccc4C3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221712 91122 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 640 9 2 6 5.7 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN3CCc4ccccc4C3)CC2)c2ccccc12 10.1021/jm061118e
16105865 176120 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 494 7 2 5 3.9 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccnc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL441870 176120 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 494 7 2 5 3.9 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccnc3C)c3ccccc23)CC1 10.1021/jm061118e
16065567 205605 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 419 3 0 4 4.3 CC1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccncc3)CC4)cccc2O1 10.1021/jm900713y
CHEMBL583621 205605 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 419 3 0 4 4.3 CC1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccncc3)CC4)cccc2O1 10.1021/jm900713y
10479253 98314 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 457 5 1 6 4.3 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2n1 10.1016/j.bmcl.2006.12.076
CHEMBL240461 98314 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 457 5 1 6 4.3 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2n1 10.1016/j.bmcl.2006.12.076
44439883 100618 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 468 5 0 6 5.0 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc6ccccc6n5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247761 100618 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 468 5 0 6 5.0 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc6ccccc6n5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
10412437 158108 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 470 5 0 6 4.9 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6n5C)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL396102 158108 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 470 5 0 6 4.9 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6n5C)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
11951000 104598 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2cc[n+]([O-])cc2)CC3)c1 10.1021/jm900713y
CHEMBL272022 104598 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2cc[n+]([O-])cc2)CC3)c1 10.1021/jm900713y
44457093 104554 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 441 5 0 4 5.4 O=C(c1ccncc1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm070543k
CHEMBL271768 104554 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 441 5 0 4 5.4 O=C(c1ccncc1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm070543k
11951000 104598 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2cc[n+]([O-])cc2)CC3)c1 10.1021/jm070543k
CHEMBL272022 104598 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2cc[n+]([O-])cc2)CC3)c1 10.1021/jm070543k
44457105 165393 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 504 6 0 4 6.7 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccc(Cl)cc1)CC2 10.1021/jm070543k
CHEMBL409224 165393 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 504 6 0 4 6.7 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccc(Cl)cc1)CC2 10.1021/jm070543k
44457105 165393 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 504 6 0 4 6.7 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccc(Cl)cc1)CC2 10.1021/jm900713y
CHEMBL409224 165393 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 504 6 0 4 6.7 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccc(Cl)cc1)CC2 10.1021/jm900713y
16105775 90163 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 549 11 2 4 5.9 CCCCCc1ccc(C(=O)Nc2ccc(S(=O)(=O)NC3CCN(C(=O)CCC)CC3)c3ccccc23)cc1 10.1021/jm061118e
CHEMBL219431 90163 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 549 11 2 4 5.9 CCCCCc1ccc(C(=O)Nc2ccc(S(=O)(=O)NC3CCN(C(=O)CCC)CC3)c3ccccc23)cc1 10.1021/jm061118e
16105868 144819 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 471 7 2 4 4.0 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL376517 144819 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 471 7 2 4 4.0 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCCC3)c3ccccc23)CC1 10.1021/jm061118e
16105867 144644 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 443 7 2 4 3.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL376071 144644 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 443 7 2 4 3.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CC3)c3ccccc23)CC1 10.1021/jm061118e
16105863 91106 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 539 7 2 6 4.2 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc(C(C)(C)C)nn3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221650 91106 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 539 7 2 6 4.2 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc(C(C)(C)C)nn3C)c3ccccc23)CC1 10.1021/jm061118e
10003657 159609 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 445 5 0 5 5.0 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(C)c(C)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL397395 159609 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 445 5 0 5 5.0 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(C)c(C)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
11685733 146980 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 589 9 2 5 6.1 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL380492 146980 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 589 9 2 5 6.1 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
16105817 143750 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 578 9 2 6 4.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN3CCCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL374527 143750 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 578 9 2 6 4.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN3CCCC3)CC2)c2ccccc12 10.1021/jm061118e
44598058 204911 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 472 6 0 6 4.8 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccncn2)CC3)c1 10.1021/jm900713y
CHEMBL574655 204911 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 472 6 0 6 4.8 COc1ccccc1Oc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccncn2)CC3)c1 10.1021/jm900713y
16105781 89935 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 480 7 2 5 3.6 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccn3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218298 89935 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 480 7 2 5 3.6 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccn3)c3ccccc23)CC1 10.1021/jm061118e
11526626 82317 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 531 8 1 4 6.3 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL204419 82317 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 531 8 1 4 6.3 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
16105779 143979 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 528 7 2 5 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc(C)nc(Cl)c3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL374964 143979 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 528 7 2 5 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc(C)nc(Cl)c3)c3ccccc23)CC1 10.1021/jm061118e
16105778 89372 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 551 7 2 5 5.1 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc(C)oc3C(F)(F)F)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL217909 89372 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 551 7 2 5 5.1 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cc(C)oc3C(F)(F)F)c3ccccc23)CC1 10.1021/jm061118e
16105858 91135 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccc(C)c3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221790 91135 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccc(C)c3)c3ccccc23)CC1 10.1021/jm061118e
44598062 204049 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 446 3 1 5 4.4 CC1(C)C=Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccnc(N)c3)CC4)c2O1 10.1021/jm900713y
CHEMBL568522 204049 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 446 3 1 5 4.4 CC1(C)C=Cc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccnc(N)c3)CC4)c2O1 10.1021/jm900713y
10255258 157247 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 495 5 0 5 5.2 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(Br)cc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL395424 157247 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 495 5 0 5 5.2 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(Br)cc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
16112836 100140 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR8 expressed in HUT78 cells assessed as I309-mediated migration by chemotaxis assayAntagonist activity at human recombinant CCR8 expressed in HUT78 cells assessed as I309-mediated migration by chemotaxis assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc([C@@H]3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL245568 100140 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR8 expressed in HUT78 cells assessed as I309-mediated migration by chemotaxis assayAntagonist activity at human recombinant CCR8 expressed in HUT78 cells assessed as I309-mediated migration by chemotaxis assay
ChEMBL 456 5 1 5 4.9 COc1ccc2nccc([C@@H]3CN(C4CCN(Cc5cc6ccccc6[nH]5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
10409369 176284 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 411 8 0 5 4.8 CCCCCCN1CCC(N2CC(c3ccnc4ccc(OC)cc34)OC2=O)CC1 10.1016/j.bmcl.2006.12.076
CHEMBL443315 176284 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 411 8 0 5 4.8 CCCCCCN1CCC(N2CC(c3ccnc4ccc(OC)cc34)OC2=O)CC1 10.1016/j.bmcl.2006.12.076
44598820 205560 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 465 6 0 4 4.8 O=C(c1ccncc1)N1CCC2(CCN(Cc3ccccc3OC(F)(F)C(F)F)CC2)CC1 10.1021/jm900713y
CHEMBL583212 205560 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 465 6 0 4 4.8 O=C(c1ccncc1)N1CCC2(CCN(Cc3ccccc3OC(F)(F)C(F)F)CC2)CC1 10.1021/jm900713y
11965686 205634 2 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 487 6 1 5 4.7 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccc[nH]c1=O)CC2 10.1021/jm900713y
CHEMBL583843 205634 2 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 487 6 1 5 4.7 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccc[nH]c1=O)CC2 10.1021/jm900713y
11539239 84901 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 430 8 1 4 4.8 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)Cc3ccccc3)CC2)c1 10.1021/jm050965z
CHEMBL210322 84901 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 430 8 1 4 4.8 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)Cc3ccccc3)CC2)c1 10.1021/jm050965z
11519336 84651 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 527 9 1 5 5.6 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4OC)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL209350 84651 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
ChEMBL 527 9 1 5 5.6 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4OC)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
16105783 89986 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 457 7 2 4 3.6 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218554 89986 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 457 7 2 4 3.6 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCC3)c3ccccc23)CC1 10.1021/jm061118e
16105773 91185 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 497 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221978 91185 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 497 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1021/jm061118e
16105784 91095 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 485 7 2 4 4.4 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCCCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221586 91095 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 485 7 2 4 4.4 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C3CCCCC3)c3ccccc23)CC1 10.1021/jm061118e
16065704 205652 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 436 3 1 6 3.7 CC1(C)Oc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccnc(N)c3)CC4)c2O1 10.1021/jm900713y
CHEMBL584087 205652 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 436 3 1 6 3.7 CC1(C)Oc2cccc(CN3CCC4(CC3)CCN(C(=O)c3ccnc(N)c3)CC4)c2O1 10.1021/jm900713y
16105861 89934 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 535 7 2 4 5.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(C(C)(C)C)cc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218297 89934 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 535 7 2 4 5.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(C(C)(C)C)cc3)c3ccccc23)CC1 10.1021/jm061118e
16105787 90688 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 473 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)CC(C)(C)C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL220651 90688 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 473 7 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)CC(C)(C)C)c3ccccc23)CC1 10.1021/jm061118e
10343818 158137 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 451 5 0 5 5.1 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(Cl)cc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL396124 158137 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 451 5 0 5 5.1 COc1ccc2nccc(C3CN(C4CCN(Cc5ccc(Cl)cc5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439838 98138 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 8 1 5 4.7 COc1ccc2nccc(C3CN(CCCN(C)Cc4cc5ccccc5[nH]4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL240249 98138 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 8 1 5 4.7 COc1ccc2nccc(C3CN(CCCN(C)Cc4cc5ccccc5[nH]4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439887 100689 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 451 5 0 5 5.1 COc1ccc2nccc(C3CN(C4CCN(Cc5cccc(Cl)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL248169 100689 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 451 5 0 5 5.1 COc1ccc2nccc(C3CN(C4CCN(Cc5cccc(Cl)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439909 174308 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 499 4 0 5 5.3 COc1ccc2nccc(C3CN(C4CCN(C(=O)c5ccc(Cl)c(Cl)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL430012 174308 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 499 4 0 5 5.3 COc1ccc2nccc(C3CN(C4CCN(C(=O)c5ccc(Cl)c(Cl)c5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
16105786 148485 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 473 9 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C(CC)CC)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL385654 148485 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 473 9 2 4 4.3 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C(CC)CC)c3ccccc23)CC1 10.1021/jm061118e
16105856 90689 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 521 9 2 4 5.0 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C(CC)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL220652 90689 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 521 9 2 4 5.0 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)C(CC)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
44598819 203771 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 419 6 0 4 4.6 C=C(C)COc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm900713y
CHEMBL566759 203771 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 419 6 0 4 4.6 C=C(C)COc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1ccncc1)CC2 10.1021/jm900713y
11950827 104396 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1cccc[n+]1[O-])CC2 10.1021/jm070543k
CHEMBL270969 104396 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 487 6 0 5 4.6 COc1ccccc1Oc1ccccc1CN1CCC2(CC1)CCN(C(=O)c1cccc[n+]1[O-])CC2 10.1021/jm070543k
10412573 100576 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 473 5 0 6 5.6 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6s5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247564 100576 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 473 5 0 6 5.6 COc1ccc2nccc(C3CN(C4CCN(Cc5cc6ccccc6s5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
44439885 100650 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 423 5 0 5 4.8 COc1ccc2nccc(C3CN(C4CCN(CC5CCCCC5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
CHEMBL247963 100650 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 423 5 0 5 4.8 COc1ccc2nccc(C3CN(C4CCN(CC5CCCCC5)CC4)C(=O)O3)c2c1 10.1016/j.bmcl.2006.12.076
16065569 203746 25 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2O1 10.1021/jm900713y
CHEMBL566543 203746 25 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 434 3 1 5 3.9 CC1(C)Cc2c(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)cccc2O1 10.1021/jm900713y
11273324 102683 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm070543k
CHEMBL259243 102683 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR8 receptorAntagonist activity at CCR8 receptor
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm070543k
11273324 102683 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm900713y
CHEMBL259243 102683 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 474 5 0 3 6.7 O=C(c1ccc(Cl)cc1)N1CCC2(CCN(Cc3ccccc3Oc3ccccc3)CC2)CC1 10.1021/jm900713y
16105866 89987 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 480 7 2 5 3.6 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccnc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218555 89987 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 480 7 2 5 3.6 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3cccnc3)c3ccccc23)CC1 10.1021/jm061118e
16105771 91333 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(C)cc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL222062 91333 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccc(C)cc3)c3ccccc23)CC1 10.1021/jm061118e
16105815 89953 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 552 9 2 6 4.2 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN(C)C)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL218369 89953 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assayAntagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
ChEMBL 552 9 2 6 4.2 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)OCCCN(C)C)CC2)c2ccccc12 10.1021/jm061118e
44598061 203817 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 448 3 1 5 4.3 CC1(C)CCc2cc(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)ccc2O1 10.1021/jm900713y
CHEMBL567202 203817 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR8Antagonist activity at human CCR8
ChEMBL 448 3 1 5 4.3 CC1(C)CCc2cc(CN3CCC4(CC3)CCN(C(=O)c3ccc(N)cn3)CC4)ccc2O1 10.1021/jm900713y
15664 90563 101 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
Drug Central 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 None
CHEMBL2205807 90563 101 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis
Drug Central 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 None
486830 10774 0 None -10 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10419462
768 10774 0 None -10 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10419462
812 7611 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10419462
812 7611 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11154210
812 7611 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16221874
815 10773 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10419462
815 10773 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11154210
816 10772 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10419462
11688990 10919 0 None - 1 Human 5.7 pIC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 9 1 5 2.6 OCCOCCN1CCN(CC1)Cc1cccc(c1)Oc1ccccc1 16221874
813 10919 0 None - 1 Human 5.7 pIC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 9 1 5 2.6 OCCOCCN1CCN(CC1)Cc1cccc(c1)Oc1ccccc1 16221874
CHEMBL1883966 10919 0 None - 1 Human 5.7 pIC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 356 9 1 5 2.6 OCCOCCN1CCN(CC1)Cc1cccc(c1)Oc1ccccc1 16221874




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
CHEMBL5268017 200323 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin)
ChEMBL 471 8 1 5 4.5 COc1ccccc1Oc1cccc(CN2CCC3(CC2)C(=O)NCN3CCc2ccccc2)c1 10.1021/acs.jmedchem.6b01309
CHEMBL5277802 200729 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin)
ChEMBL 527 11 1 5 5.8 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C(CCN3CCCC3)c3ccccc3)CC2)c1 10.1021/acs.jmedchem.6b01309
CHEMBL5272687 200511 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin)
ChEMBL 526 10 2 7 4.3 CCNS(=O)(=O)c1ccc(OC)cc1C1(O)CCN(Cc2cccc(Oc3ccccc3OC)c2)CC1 10.1021/acs.jmedchem.6b01309
CHEMBL5270110 200398 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin)
ChEMBL 433 7 2 5 4.7 COc1ccccc1Oc1cccc(CN2CCC(O)(c3ccccc3C(=O)O)CC2)c1 10.1021/acs.jmedchem.6b01309
CHEMBL5273480 200546 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin)
ChEMBL 485 7 2 5 4.7 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3CC(=O)Nc4ccccc43)CC2)c1 10.1021/acs.jmedchem.6b01309
155557362 181422 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at human CCR8 expressed in CHOK1 cells assessed as reduction in CCL1-induced beta-arrestin 2 recruitment incubated for 30 mins followed by CCL1 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human CCR8 expressed in CHOK1 cells assessed as reduction in CCL1-induced beta-arrestin 2 recruitment incubated for 30 mins followed by CCL1 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 560 6 1 6 5.4 CC[C@]12C=C(C(=O)OC)n3c(c(CCNC(=O)c4ccc(Br)cc4)c4ccccc43)[C@H]1N(C#N)CCC2 10.1021/acs.jmedchem.9b01924
CHEMBL4558185 181422 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at human CCR8 expressed in CHOK1 cells assessed as reduction in CCL1-induced beta-arrestin 2 recruitment incubated for 30 mins followed by CCL1 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human CCR8 expressed in CHOK1 cells assessed as reduction in CCL1-induced beta-arrestin 2 recruitment incubated for 30 mins followed by CCL1 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 560 6 1 6 5.4 CC[C@]12C=C(C(=O)OC)n3c(c(CCNC(=O)c4ccc(Br)cc4)c4ccccc43)[C@H]1N(C#N)CCC2 10.1021/acs.jmedchem.9b01924
132072454 186503 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CCR8 expressed in CHO-K1 cells by PathHunter beta-arrestin assayAntagonist activity at human CCR8 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 186503 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CCR8 expressed in CHO-K1 cells by PathHunter beta-arrestin assayAntagonist activity at human CCR8 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
10367938 89954 0 None - 1 Human 9.8 pKi = 9.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 2 5 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218374 89954 0 None - 1 Human 9.8 pKi = 9.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 2 5 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
10391001 143976 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL374939 143976 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 493 7 2 4 4.5 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
11754900 91141 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 480 5 3 4 3.5 CNC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221865 91141 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 480 5 3 4 3.5 CNC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
10006907 148592 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 520 6 3 5 3.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)[C@@H]3CCCN3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL386308 148592 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 520 6 3 5 3.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)[C@@H]3CCCN3)CC2)c2ccccc12 10.1021/jm061118e
10006907 148592 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 520 6 3 5 3.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)[C@@H]3CCCN3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL386308 148592 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 520 6 3 5 3.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)[C@@H]3CCCN3)CC2)c2ccccc12 10.1021/jm061118e
9984180 143327 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 520 5 2 4 4.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL373739 143327 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 520 5 2 4 4.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCCC3)CC2)c2ccccc12 10.1021/jm061118e
16105811 144447 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 506 6 3 5 2.9 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)C3CNC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL375854 144447 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 506 6 3 5 2.9 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)C3CNC3)CC2)c2ccccc12 10.1021/jm061118e
16105788 89955 9 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 6 2 5 4.3 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL218375 89955 9 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 6 2 5 4.3 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
16105880 91143 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 508 8 3 5 3.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCCN)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221867 91143 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 508 8 3 5 3.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCCN)CC2)c2ccccc12 10.1021/jm061118e
16105822 144937 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 494 5 2 4 3.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N(C)C)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL376910 144937 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 494 5 2 4 3.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N(C)C)CC2)c2ccccc12 10.1021/jm061118e
16105890 148724 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 542 6 3 4 5.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)Nc3ccccc3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL387161 148724 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 542 6 3 4 5.4 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)Nc3ccccc3)CC2)c2ccccc12 10.1021/jm061118e
11519336 84651 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 527 9 1 5 5.6 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4OC)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL209350 84651 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 527 9 1 5 5.6 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4OC)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
16105807 90747 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 494 7 3 5 3.0 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCN)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL220703 90747 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 494 7 3 5 3.0 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCN)CC2)c2ccccc12 10.1021/jm061118e
16105813 91020 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 570 7 2 5 5.1 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221078 91020 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 570 7 2 5 5.1 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)c3ccc(N(C)C)cc3)CC2)c2ccccc12 10.1021/jm061118e
16105831 90189 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 488 5 2 5 3.8 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)N3CCCCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL219589 90189 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 488 5 2 5 3.8 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)N3CCCCC3)c3ccccc23)CC1 10.1021/jm061118e
11502217 82810 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 400 7 1 3 4.8 O=C(Cc1ccccc1)NC1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
CHEMBL205692 82810 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 400 7 1 3 4.8 O=C(Cc1ccccc1)NC1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
11526626 82317 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 531 8 1 4 6.3 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL204419 82317 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 531 8 1 4 6.3 CCN1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
16105760 144645 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 509 5 2 5 4.8 CC(C)(C)OC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL376076 144645 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 509 5 2 5 4.8 CC(C)(C)OC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
16105805 91179 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 7 2 5 3.3 COCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221961 91179 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 7 2 5 3.3 COCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
16105799 172925 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 482 6 1 6 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(OC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL426207 172925 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 482 6 1 6 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(OC(=O)c3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
11774008 91374 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 402 5 2 3 4.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)c2ccccc12)c1ccccc1 10.1021/jm061118e
CHEMBL222110 91374 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 402 5 2 3 4.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)c2ccccc12)c1ccccc1 10.1021/jm061118e
16105809 91103 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 522 9 3 5 3.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCCCN)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221638 91103 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 522 9 3 5 3.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCCCN)CC2)c2ccccc12 10.1021/jm061118e
16105889 90746 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 494 6 3 4 3.9 CCNC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL220701 90746 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 494 6 3 4 3.9 CCNC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
9982672 89600 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 2 5 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2cccc3c(NC(=O)c4ccccc4)cccc23)CC1 10.1021/jm061118e
CHEMBL218037 89600 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 2 5 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2cccc3c(NC(=O)c4ccccc4)cccc23)CC1 10.1021/jm061118e
16105802 90840 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 479 6 2 4 4.1 CCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL220753 90840 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 479 6 2 4 4.1 CCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
16105895 148696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 2 5 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc3cccc(NC(=O)c4ccccc4)c3c2)CC1 10.1021/jm061118e
CHEMBL386987 148696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 2 5 4.0 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc3cccc(NC(=O)c4ccccc4)c3c2)CC1 10.1021/jm061118e
11563243 175479 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 575 9 2 5 5.7 CCN1CCC(C(=O)NC2(C(=O)O)CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL436753 175479 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 575 9 2 5 5.7 CCN1CCC(C(=O)NC2(C(=O)O)CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
11270007 91375 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 416 6 2 3 4.6 O=C(Nc1ccc(S(=O)(=O)NCc2ccccc2)c2ccccc12)c1ccccc1 10.1021/jm061118e
CHEMBL222111 91375 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 416 6 2 3 4.6 O=C(Nc1ccc(S(=O)(=O)NCc2ccccc2)c2ccccc12)c1ccccc1 10.1021/jm061118e
16105888 143152 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 466 5 3 4 3.2 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(N)=O)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL373504 143152 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 466 5 3 4 3.2 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(N)=O)CC2)c2ccccc12 10.1021/jm061118e
11541073 82765 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 532 8 1 4 7.1 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccc(Cl)cc4)CCCCC3)CC2)c1 10.1021/jm050965z
CHEMBL205457 82765 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 532 8 1 4 7.1 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccc(Cl)cc4)CCCCC3)CC2)c1 10.1021/jm050965z
11539239 84901 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 430 8 1 4 4.8 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)Cc3ccccc3)CC2)c1 10.1021/jm050965z
CHEMBL210322 84901 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 430 8 1 4 4.8 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)Cc3ccccc3)CC2)c1 10.1021/jm050965z
792361 82966 7 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 339 6 0 4 4.3 CCOC(=O)C1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
CHEMBL205808 82966 7 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 339 6 0 4 4.3 CCOC(=O)C1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
11584004 147476 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 489 7 2 4 5.1 O=C(NC1CCN(Cc2cccc(Oc3ccccc3Cl)c2)CC1)C1(c2ccccc2)CCNC1 10.1021/jm050965z
CHEMBL381619 147476 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 489 7 2 4 5.1 O=C(NC1CCN(Cc2cccc(Oc3ccccc3Cl)c2)CC1)C1(c2ccccc2)CCNC1 10.1021/jm050965z
16105891 91026 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 506 5 2 4 4.0 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221130 91026 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 506 5 2 4 4.0 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCC3)CC2)c2ccccc12 10.1021/jm061118e
44419035 91056 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 9 2 5 4.8 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NCCCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221345 91056 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 9 2 5 4.8 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NCCCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
11384528 148410 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 417 6 2 4 4.0 O=C(Nc1ccc(S(=O)(=O)NCc2ccncc2)c2ccccc12)c1ccccc1 10.1021/jm061118e
CHEMBL385287 148410 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 417 6 2 4 4.0 O=C(Nc1ccc(S(=O)(=O)NCc2ccncc2)c2ccccc12)c1ccccc1 10.1021/jm061118e
16105832 90136 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 479 7 2 4 4.1 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)C1 10.1021/jm061118e
CHEMBL219327 90136 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 479 7 2 4 4.1 CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)C1 10.1021/jm061118e
44419032 91332 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 8 2 5 4.4 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NCCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL222058 91332 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 8 2 5 4.4 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NCCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
16105840 91134 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 468 7 1 5 4.3 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(OCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221789 91134 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 468 7 1 5 4.3 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(OCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
10254576 91151 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 480 6 3 5 2.6 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CN)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221904 91151 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 480 6 3 5 2.6 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CN)CC2)c2ccccc12 10.1021/jm061118e
16105824 91045 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 549 5 2 5 3.5 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCN(C)CC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL221251 91045 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 549 5 2 5 3.5 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCN(C)CC3)CC2)c2ccccc12 10.1021/jm061118e
16105892 148385 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 534 5 2 4 4.7 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCCCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL385108 148385 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 534 5 2 4 4.7 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCCCC3)CC2)c2ccccc12 10.1021/jm061118e
11452569 89976 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 408 5 2 3 4.7 O=C(Nc1ccc(S(=O)(=O)NC2CCCCC2)c2ccccc12)c1ccccc1 10.1021/jm061118e
CHEMBL218503 89976 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 408 5 2 3 4.7 O=C(Nc1ccc(S(=O)(=O)NC2CCCCC2)c2ccccc12)c1ccccc1 10.1021/jm061118e
3384970 168060 8 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 432 6 2 4 4.9 COc1ccc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)cc1 10.1021/jm061118e
CHEMBL412116 168060 8 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 432 6 2 4 4.9 COc1ccc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)c3ccccc23)cc1 10.1021/jm061118e
44419031 144480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 467 7 2 5 4.4 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL375880 144480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 467 7 2 5 4.4 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(NCc3ccccc3)c3ccccc23)CC1 10.1021/jm061118e
10391077 144162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 6 2 5 4.3 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(C(=O)Nc3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL375315 144162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 495 6 2 5 4.3 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(C(=O)Nc3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
16105877 89599 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 3 5 2.7 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CO)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL218036 89599 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 481 6 3 5 2.7 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CO)CC2)c2ccccc12 10.1021/jm061118e
16105844 89546 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 465 7 2 4 3.7 CCCC(=O)N1CC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)C1 10.1021/jm061118e
CHEMBL217979 89546 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 465 7 2 4 3.7 CCCC(=O)N1CC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)C1 10.1021/jm061118e
16105830 90173 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 564 11 2 5 4.8 CCN(CC)CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL219487 90173 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 564 11 2 5 4.8 CCN(CC)CCCC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
11235229 90188 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 409 5 3 4 3.1 O=C(Nc1ccc(S(=O)(=O)NC2CCNCC2)c2ccccc12)c1ccccc1 10.1021/jm061118e
CHEMBL219588 90188 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 409 5 3 4 3.1 O=C(Nc1ccc(S(=O)(=O)NC2CCNCC2)c2ccccc12)c1ccccc1 10.1021/jm061118e
11541506 83291 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 575 9 2 5 5.7 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)C1 10.1021/jm050965z
CHEMBL205993 83291 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 575 9 2 5 5.7 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)C1 10.1021/jm050965z
16105893 89922 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 536 5 2 5 3.6 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCOCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL218218 89922 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 536 5 2 5 3.6 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)N3CCOCC3)CC2)c2ccccc12 10.1021/jm061118e
16105803 91184 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 465 5 2 4 3.7 CC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221977 91184 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 465 5 2 4 3.7 CC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
11706579 146515 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 543 9 3 6 4.3 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)(C(=O)O)CC2)c1 10.1021/jm050965z
CHEMBL379834 146515 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 543 9 3 6 4.3 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)(C(=O)O)CC2)c1 10.1021/jm050965z
11533398 82761 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 499 8 2 5 4.9 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)CC2)c1 10.1021/jm050965z
CHEMBL205447 82761 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 499 8 2 5 4.9 COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)CC2)c1 10.1021/jm050965z
16105876 143982 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 491 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)C3CC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL374979 143982 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 491 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)C3CC3)CC2)c2ccccc12 10.1021/jm061118e
16105826 89951 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 578 9 2 6 3.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCCN3CCOCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL218366 89951 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 578 9 2 6 3.8 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)CCCN3CCOCC3)CC2)c2ccccc12 10.1021/jm061118e
16105820 148411 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 508 7 3 4 4.3 CCCNC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL385288 148411 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 508 7 3 4 4.3 CCCNC(=O)N1CCC(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c3ccccc23)CC1 10.1021/jm061118e
16105821 89947 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 508 6 3 4 4.3 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)NC(C)C)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL218350 89947 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 508 6 3 4 4.3 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)NC(C)C)CC2)c2ccccc12 10.1021/jm061118e
1099153 89917 10 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 396 4 1 4 3.1 O=C(Nc1ccc(S(=O)(=O)N2CCOCC2)c2ccccc12)c1ccccc1 10.1021/jm061118e
CHEMBL218207 89917 10 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 396 4 1 4 3.1 O=C(Nc1ccc(S(=O)(=O)N2CCOCC2)c2ccccc12)c1ccccc1 10.1021/jm061118e
16105882 148773 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 527 6 2 4 5.0 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)c3ccccc3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL387451 148773 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 527 6 2 4 5.0 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)c3ccccc3)CC2)c2ccccc12 10.1021/jm061118e
11685733 146980 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 589 9 2 5 6.1 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
CHEMBL380492 146980 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 589 9 2 5 6.1 CC(C)(C(=O)O)N1CCC(C(=O)NC2CCN(Cc3cccc(Oc4ccccc4Cl)c3)CC2)(c2ccccc2)CC1 10.1021/jm050965z
16105804 90165 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 519 6 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)C3CCCC3)CC2)c2ccccc12 10.1021/jm061118e
CHEMBL219433 90165 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 519 6 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC2CCN(C(=O)C3CCCC3)CC2)c2ccccc12 10.1021/jm061118e
11329260 91014 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 487 6 2 5 3.8 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(C(=O)NC3CCCCC3)c3ccccc23)CC1 10.1021/jm061118e
CHEMBL221021 91014 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assayBinding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL 487 6 2 5 3.8 CCOC(=O)N1CCC(NS(=O)(=O)c2ccc(C(=O)NC3CCCCC3)c3ccccc23)CC1 10.1021/jm061118e
11530171 82745 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 338 6 1 3 3.8 CCNC(=O)C1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
CHEMBL205304 82745 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 338 6 1 3 3.8 CCNC(=O)C1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
11681610 147363 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 338 6 1 3 4.0 CCC(=O)NC1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z
CHEMBL381354 147363 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cellsDisplacement of [125I]I309 from human CCR8 expressed in L1.2 cells
ChEMBL 338 6 1 3 4.0 CCC(=O)NC1CCN(Cc2cccc(Oc3ccccc3)c2)CC1 10.1021/jm050965z