Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
ID		 Reference
ligand		 Vendors

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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
93149 107257 None 55 Human Functional pEC50 = 6 6.0 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
CHEMBL316589 107257 None 55 Human Functional pEC50 = 6 6.0 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
336912 83817 None 20 Human Functional pEC50 = 5 5.0 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 240 2 2 4 1.8 OCc1ccc2ccc3ccc(CO)nc3c2n1 10.1021/jm301121j
CHEMBL2205802 83817 None 20 Human Functional pEC50 = 5 5.0 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 240 2 2 4 1.8 OCc1ccc2ccc3ccc(CO)nc3c2n1 10.1021/jm301121j
2733927 83822 None 59 Human Functional pEC50 = 5 5.0 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83822 None 59 Human Functional pEC50 = 5 5.0 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
667748 83819 None 57 Human Functional pEC50 = 5.9 5.9 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83819 None 57 Human Functional pEC50 = 5.9 5.9 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
20445 83820 None 65 Human Functional pEC50 = 4.9 4.9 -2 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83820 None 65 Human Functional pEC50 = 4.9 4.9 -2 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
667748 83819 None 57 Human Functional pEC50 = 5.9 5.9 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83819 None 57 Human Functional pEC50 = 5.9 5.9 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
15783796 83825 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
CHEMBL2205810 83825 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
602123 83818 None 43 Human Functional pEC50 = 4.9 4.9 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
CHEMBL2205803 83818 None 43 Human Functional pEC50 = 4.9 4.9 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
20445 83820 None 65 Human Functional pEC50 = 4.9 4.9 -2 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83820 None 65 Human Functional pEC50 = 4.9 4.9 -2 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
15783796 83825 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
CHEMBL2205810 83825 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
602123 83818 None 43 Human Functional pEC50 = 4.9 4.9 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
CHEMBL2205803 83818 None 43 Human Functional pEC50 = 4.9 4.9 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
74265 210806 None 69 Human Functional pEC50 = 5.8 5.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 210806 None 69 Human Functional pEC50 = 5.8 5.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
353741 72088 None 4 Human Functional pEC50 = 4.8 4.8 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 364 2 0 2 4.6 BrCc1ccc2ccc3ccc(CBr)nc3c2n1 10.1021/jm301121j
CHEMBL1976682 72088 None 4 Human Functional pEC50 = 4.8 4.8 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 364 2 0 2 4.6 BrCc1ccc2ccc3ccc(CBr)nc3c2n1 10.1021/jm301121j
65237 137711 None 68 Human Functional pEC50 = 5.8 5.8 28 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
CHEMBL375781 137711 None 68 Human Functional pEC50 = 5.8 5.8 28 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
74265 210806 None 69 Human Functional pEC50 = 5.8 5.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 210806 None 69 Human Functional pEC50 = 5.8 5.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
353741 72088 None 4 Human Functional pEC50 = 4.8 4.8 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 364 2 0 2 4.6 BrCc1ccc2ccc3ccc(CBr)nc3c2n1 10.1021/jm301121j
CHEMBL1976682 72088 None 4 Human Functional pEC50 = 4.8 4.8 - 1
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 364 2 0 2 4.6 BrCc1ccc2ccc3ccc(CBr)nc3c2n1 10.1021/jm301121j
15664 83821 None 63 Human Functional pEC50 = 4.8 4.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83821 None 63 Human Functional pEC50 = 4.8 4.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
65237 137711 None 68 Human Functional pEC50 = 5.8 5.8 28 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
CHEMBL375781 137711 None 68 Human Functional pEC50 = 5.8 5.8 28 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
15664 83821 None 63 Human Functional pEC50 = 4.8 4.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83821 None 63 Human Functional pEC50 = 4.8 4.8 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
72791 210699 None 48 Human Functional pEC50 = 5.8 5.8 1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL98682 210699 None 48 Human Functional pEC50 = 5.8 5.8 1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
77865 107342 None 51 Human Functional pEC50 = 5.7 5.7 -1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL317115 107342 None 51 Human Functional pEC50 = 5.7 5.7 -1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
72791 210699 None 48 Human Functional pEC50 = 5.7 5.7 1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL98682 210699 None 48 Human Functional pEC50 = 5.7 5.7 1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cc2cccnc2c2ncccc12 10.1021/jm301121j
12041800 205951 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopyAgonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopy
ChEMBL 410 7 2 4 6.4 Clc1ccc2c(NCCCCNc3ccnc4cc(Cl)ccc34)ccnc2c1 10.1016/j.bmcl.2011.11.014
CHEMBL66165 205951 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopyAgonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopy
ChEMBL 410 7 2 4 6.4 Clc1ccc2c(NCCCCNc3ccnc4cc(Cl)ccc34)ccnc2c1 10.1016/j.bmcl.2011.11.014
77865 107342 None 51 Human Functional pEC50 = 5.7 5.7 -1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL317115 107342 None 51 Human Functional pEC50 = 5.7 5.7 -1 2
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
1474 154488 None 79 Human Functional pEC50 = 4.5 4.5 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
CHEMBL39879 154488 None 79 Human Functional pEC50 = 4.5 4.5 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
1474 154488 None 79 Human Functional pEC50 = 4.5 4.5 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
CHEMBL39879 154488 None 79 Human Functional pEC50 = 4.5 4.5 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
14338 4369 None 74 Human Functional pEC50 = 5.4 5.4 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 4369 None 74 Human Functional pEC50 = 5.4 5.4 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
14338 4369 None 74 Human Functional pEC50 = 5.4 5.4 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 4369 None 74 Human Functional pEC50 = 5.4 5.4 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
12987698 83823 None 3 Human Functional pEC50 = 5.3 5.3 -2 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83823 None 3 Human Functional pEC50 = 5.3 5.3 -2 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
14434082 83816 None 16 Human Functional pEC50 = 5.3 5.3 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83816 None 16 Human Functional pEC50 = 5.3 5.3 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83816 None 16 Human Functional pEC50 = 5.3 5.3 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83816 None 16 Human Functional pEC50 = 5.3 5.3 1 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
12987698 83823 None 3 Human Functional pEC50 = 5.3 5.3 -2 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83823 None 3 Human Functional pEC50 = 5.3 5.3 -2 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
12425 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
12425 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 6 None 76 Human Functional pEC50 = 5.2 5.2 -5 4
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
70848 209130 None 67 Human Functional pEC50 = 4.2 4.2 -12 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 209130 None 67 Human Functional pEC50 = 4.2 4.2 -12 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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
70848 209130 None 67 Human Functional pEC50 = 4.2 4.2 -12 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 209130 None 67 Human Functional pEC50 = 4.2 4.2 -12 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 202179 None 52 Human Functional pEC50 = 6.1 6.1 -7 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 202179 None 52 Human Functional pEC50 = 6.1 6.1 -7 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
72792 202179 None 52 Human Functional pEC50 = 6.1 6.1 -7 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 202179 None 52 Human Functional pEC50 = 6.1 6.1 -7 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
11151928 189596 None 0 Human Functional pED50 = 9.8 9.8 -1 4
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL513863 189596 None 0 Human Functional pED50 = 9.8 9.8 -1 4
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
10456104 72006 None 0 Human Functional pIC50 = 10 10.0 56 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197375 72006 None 0 Human Functional pIC50 = 10 10.0 56 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
59278332 171175 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 7 3.2 CCC(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4457209 171175 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 7 3.2 CCC(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
59278286 171658 None 1 Human Functional pIC50 = 9.7 9.7 112 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4464625 171658 None 1 Human Functional pIC50 = 9.7 9.7 112 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
45138759 172440 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 467 7 1 7 3.6 CCCC(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4475581 172440 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 467 7 1 7 3.6 CCCC(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
512282 758 None 42 Human Functional pIC50 = 9.4 9.4 141 5
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
767 758 None 42 Human Functional pIC50 = 9.4 9.4 141 5
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
CHEMBL232656 758 None 42 Human Functional pIC50 = 9.4 9.4 141 5
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
6918497 113493 None 1 Human Functional pIC50 = 9.1 9.1 -1 4
Inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptorInhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Human Functional pIC50 = 9.1 9.1 -1 4
Inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptorInhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Human Functional pIC50 = 9.1 9.1 -1 4
Inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptorInhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
66686405 175343 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 532 5 2 5 6.3 CC(C)(O)c1ccc2c(c1)/C(=C\CCN1CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C1)c1cccnc1CO2 10.1016/j.bmcl.2018.11.015
CHEMBL4571977 175343 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 532 5 2 5 6.3 CC(C)(O)c1ccc2c(c1)/C(=C\CCN1CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C1)c1cccnc1CO2 10.1016/j.bmcl.2018.11.015
9980155 71840 None 0 Human Functional pIC50 = 9.1 9.1 23 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
CHEMBL196860 71840 None 0 Human Functional pIC50 = 9.1 9.1 23 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
10003548 71996 None 0 Human Functional pIC50 = 9 9.0 223 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197345 71996 None 0 Human Functional pIC50 = 9 9.0 223 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
11743399 72508 None 9 Human Functional pIC50 = 9 9.0 32 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL198949 72508 None 9 Human Functional pIC50 = 9 9.0 32 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44405176 135476 None 0 Human Functional pIC50 = 9 9.0 1 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL372807 135476 None 0 Human Functional pIC50 = 9 9.0 1 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
44309143 205949 None 0 Human Functional pIC50 = 9 9.0 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 481 11 4 6 2.9 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NN 10.1016/j.bmcl.2004.02.022
CHEMBL66159 205949 None 0 Human Functional pIC50 = 9 9.0 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 481 11 4 6 2.9 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NN 10.1016/j.bmcl.2004.02.022
59278147 173097 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 492 5 1 6 3.9 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cc(C(F)(F)F)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4518015 173097 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 492 5 1 6 3.9 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cc(C(F)(F)F)c1 10.1016/j.bmcl.2018.12.024
512282 758 None 42 Human Functional pIC50 = 8.9 8.9 141 5
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2018.11.015
767 758 None 42 Human Functional pIC50 = 8.9 8.9 141 5
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2018.11.015
CHEMBL232656 758 None 42 Human Functional pIC50 = 8.9 8.9 141 5
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2018.11.015
59278115 174939 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 5 1 7 2.8 CC(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4562738 174939 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 5 1 7 2.8 CC(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
512282 758 None 42 Human Functional pIC50 = 8.8 8.8 141 5
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm801416q
767 758 None 42 Human Functional pIC50 = 8.8 8.8 141 5
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm801416q
CHEMBL232656 758 None 42 Human Functional pIC50 = 8.8 8.8 141 5
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm801416q
10434371 72982 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL200629 72982 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
52916803 171085 None 20 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4456123 171085 None 20 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.1016/j.bmcl.2018.12.024
155511620 169689 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 3 6.3 CCC[C@H](NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2018.11.015
CHEMBL4436061 169689 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 3 6.3 CCC[C@H](NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2018.11.015
11554849 72877 None 0 Human Functional pIC50 = 8 8.0 2 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200242 72877 None 0 Human Functional pIC50 = 8 8.0 2 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
44453265 95439 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2007.09.068
CHEMBL256821 95439 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2007.09.068
44453400 95586 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 460 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL257509 95586 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 460 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1Cl 10.1016/j.bmcl.2007.09.068
10003548 71996 None 0 Human Functional pIC50 = 7 7.0 223 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197345 71996 None 0 Human Functional pIC50 = 7 7.0 223 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
10072252 72643 None 0 Mouse Functional pIC50 = 6 6.0 -17 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL199412 72643 None 0 Mouse Functional pIC50 = 6 6.0 -17 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44405203 72511 None 0 Human Functional pIC50 = 6 6.0 31 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
CHEMBL198966 72511 None 0 Human Functional pIC50 = 6 6.0 31 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
44405202 73019 None 0 Human Functional pIC50 = 6 6.0 17 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
CHEMBL200794 73019 None 0 Human Functional pIC50 = 6 6.0 17 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
76322249 106236 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL 880 16 6 6 11.0 CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(O)c(C(=O)NCC(=O)O)c5)c5cc(Cl)c(O)c(C(=O)NCC(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3137848 106236 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL 880 16 6 6 11.0 CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(O)c(C(=O)NCC(=O)O)c5)c5cc(Cl)c(O)c(C(=O)NCC(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138130 213578 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6cccc(C(=O)O)c6)c(C(=O)O)c5)c5cc(Cl)c(OCc6cccc(C(=O)O)c6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138370 213578 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6cccc(C(=O)O)c6)c(C(=O)O)c5)c5cc(Cl)c(OCc6cccc(C(=O)O)c6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
44453225 95791 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 440 4 1 5 3.5 O=S(=O)(c1cccs1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL258368 95791 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 440 4 1 5 3.5 O=S(=O)(c1cccs1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10003548 71996 None 0 Human Functional pIC50 = 5.0 5.0 223 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197345 71996 None 0 Human Functional pIC50 = 5.0 5.0 223 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
10789018 35185 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 435 7 1 4 5.1 N#Cc1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
CHEMBL143499 35185 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 435 7 1 4 5.1 N#Cc1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
44453503 95132 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccsc1 10.1016/j.bmcl.2007.09.068
CHEMBL255338 95132 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccsc1 10.1016/j.bmcl.2007.09.068
58138765 174519 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1cccc(F)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4552741 174519 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1cccc(F)c1 10.1016/j.bmcl.2018.12.024
44309194 205997 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 464 11 4 6 2.4 CC(C)(O)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL66457 205997 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 464 11 4 6 2.4 CC(C)(O)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
44430752 88031 None 0 Human Functional pIC50 = 7.9 7.9 147 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234295 88031 None 0 Human Functional pIC50 = 7.9 7.9 147 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44430752 88031 None 0 Human Functional pIC50 = 7.9 7.9 147 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234295 88031 None 0 Human Functional pIC50 = 7.9 7.9 147 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
59278305 170135 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 424 5 1 6 2.9 CS(=O)(=O)c1ccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4442765 170135 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 424 5 1 6 2.9 CS(=O)(=O)c1ccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
59278307 171654 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 5 1 7 3.0 CC(C)(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4464575 171654 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 5 1 7 3.0 CC(C)(NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
44470374 175980 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 507 6 1 6 3.0 CN1CCN(S(=O)(=O)c2ccc(CNC(=O)c3cccc4c3cnn4-c3ccc(F)cc3)cc2)CC1 10.1016/j.bmcl.2018.12.024
CHEMBL4586189 175980 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 507 6 1 6 3.0 CN1CCN(S(=O)(=O)c2ccc(CNC(=O)c3cccc4c3cnn4-c3ccc(F)cc3)cc2)CC1 10.1016/j.bmcl.2018.12.024
44453162 95323 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 526 4 1 4 4.6 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
CHEMBL256272 95323 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 526 4 1 4 4.6 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
44453199 95720 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 422 7 2 4 3.3 Cc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL258064 95720 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 422 7 2 4 3.3 Cc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
44469804 172121 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 424 5 1 6 2.9 CS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cn1 10.1016/j.bmcl.2018.12.024
CHEMBL4471579 172121 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 424 5 1 6 2.9 CS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cn1 10.1016/j.bmcl.2018.12.024
44405203 72511 None 0 Human Functional pIC50 = 6.9 6.9 31 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
CHEMBL198966 72511 None 0 Human Functional pIC50 = 6.9 6.9 31 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
44309407 103019 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 476 9 4 6 2.5 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCCCC1 10.1016/j.bmcl.2004.02.022
CHEMBL306457 103019 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 476 9 4 6 2.5 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCCCC1 10.1016/j.bmcl.2004.02.022
44468442 170654 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1ccccc1C(F)(F)F)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4450029 170654 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1ccccc1C(F)(F)F)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
155530458 171642 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 409 5 2 4 4.0 O=C(NCc1cccc(C(F)(F)F)c1)c1cnn(-c2ccc(Cl)cc2)c1CO 10.1016/j.bmcl.2018.11.015
CHEMBL4464403 171642 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 409 5 2 4 4.0 O=C(NCc1cccc(C(F)(F)F)c1)c1cnn(-c2ccc(Cl)cc2)c1CO 10.1016/j.bmcl.2018.11.015
44468440 173462 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 346 4 1 4 3.5 O=C(NCc1ccncc1)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4527255 173462 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 346 4 1 4 3.5 O=C(NCc1ccncc1)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4647642 216507 None 0 Human Functional pIC50 = 5.9 5.9 - 1
CCR1 cellular Ca2+-flux assayCCR1 cellular Ca2+-flux assay
ChEMBL None None None O=C([C@H]1C[C@H](O)CN1c1ccc(Cl)cc1)N1CC2COCC(C1)N2Cc1ccc(Cl)cc1 10.6019/CHEMBL4630906
44453357 97576 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 434 4 1 4 3.5 O=S(=O)(c1ccccc1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270419 97576 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 434 4 1 4 3.5 O=S(=O)(c1ccccc1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453525 97556 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 452 4 1 4 3.6 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270358 97556 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 452 4 1 4 3.6 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44309161 206500 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 462 9 3 6 2.3 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCOCC1 10.1016/j.bmcl.2004.02.022
CHEMBL69876 206500 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 462 9 3 6 2.3 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCOCC1 10.1016/j.bmcl.2004.02.022
CHEMBL3138123 213576 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CSCC[C@H](NC(=O)c1cc(C(=CCC[C@H]2CC[C@@]3(C)C(CC[C@@H]4[C@@H]3CC[C@@]3(C)[C@H]4CC[C@@H]3C(C)CCCC(C)C)C2)c2cc(Cl)c(O)c(C(=O)N[C@@H](CCSC)C(=O)O)c2)cc(Cl)c1O)C(=O)O 10.1016/s0960-894x(00)00601-6
44453638 166577 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL427834 166577 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
44430746 87151 None 0 Human Functional pIC50 = 7.9 7.9 41 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232638 87151 None 0 Human Functional pIC50 = 7.9 7.9 41 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
155564974 175581 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 5 1 3 5.9 CC[C@H](NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2018.11.015
CHEMBL4577357 175581 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 5 1 3 5.9 CC[C@H](NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2018.11.015
10388824 133506 None 0 Human Functional pIC50 = 7.9 7.9 4 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370596 133506 None 0 Human Functional pIC50 = 7.9 7.9 4 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44309397 206267 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 466 11 3 5 3.4 CC(C)(F)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL68366 206267 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 466 11 3 5 3.4 CC(C)(F)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
44453320 97542 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270253 97542 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453579 155678 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.5 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404465 155678 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.5 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44309364 206378 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 494 12 3 5 4.0 CCNC(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
CHEMBL69123 206378 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 494 12 3 5 4.0 CCNC(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
44453615 95217 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL255797 95217 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
44453402 95626 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2007.09.068
CHEMBL257698 95626 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2007.09.068
10456104 72006 None 0 Human Functional pIC50 = 5.9 5.9 56 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197375 72006 None 0 Human Functional pIC50 = 5.9 5.9 56 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44430723 86875 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 544 8 2 7 3.1 CNc1c(Nc2cc(Br)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232253 86875 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 544 8 2 7 3.1 CNc1c(Nc2cc(Br)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453614 155355 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL402825 155355 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
24758044 82895 None 0 Human Functional pIC50 = 7.8 7.8 14 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced calcium flux by FLIPRAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced calcium flux by FLIPR
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180528 82895 None 0 Human Functional pIC50 = 7.8 7.8 14 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced calcium flux by FLIPRAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced calcium flux by FLIPR
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44480600 175165 None 1 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 446 7 1 6 3.9 CCCC(NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1cncc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.11.015
CHEMBL4568048 175165 None 1 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 446 7 1 6 3.9 CCCC(NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1cncc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.11.015
44405212 72993 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 458 5 1 4 4.2 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200680 72993 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 458 5 1 4 4.2 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
10001921 72477 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
CHEMBL198852 72477 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
512282 758 None 42 Mouse Functional pIC50 = 5.8 5.8 -141 5
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
767 758 None 42 Mouse Functional pIC50 = 5.8 5.8 -141 5
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
CHEMBL232656 758 None 42 Mouse Functional pIC50 = 5.8 5.8 -141 5
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
10388824 133506 None 0 Human Functional pIC50 = 5.8 5.8 4 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370596 133506 None 0 Human Functional pIC50 = 5.8 5.8 4 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
49865900 16190 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 448 4 1 3 6.0 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCCC1c1nccn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224118 16190 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 448 4 1 3 6.0 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCCC1c1nccn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
24782574 179468 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 453 4 1 2 5.3 Cc1cc(C(F)(F)F)ccc1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL473734 179468 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 453 4 1 2 5.3 Cc1cc(C(F)(F)F)ccc1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
9980155 71840 None 0 Human Functional pIC50 = 7.8 7.8 23 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
CHEMBL196860 71840 None 0 Human Functional pIC50 = 7.8 7.8 23 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
44405234 133358 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370447 133358 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
10575889 33697 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 458 8 1 3 6.3 N#CC(CCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL142199 33697 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 458 8 1 3 6.3 N#CC(CCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
44453084 95321 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 422 6 2 3 4.6 O=C(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
CHEMBL256264 95321 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 422 6 2 3 4.6 O=C(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
44430713 86750 None 0 Human Functional pIC50 = 7.8 7.8 30 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL231829 86750 None 0 Human Functional pIC50 = 7.8 7.8 30 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
58138868 170651 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 414 4 1 4 4.5 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(F)nc1 10.1016/j.bmcl.2018.12.024
CHEMBL4449996 170651 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 414 4 1 4 4.5 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(F)nc1 10.1016/j.bmcl.2018.12.024
58138852 174169 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 452 7 2 5 3.4 CCNS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4544186 174169 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 452 7 2 5 3.4 CCNS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
58138832 169979 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 403 5 1 5 3.9 COC(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4440452 169979 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 403 5 1 5 3.9 COC(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
155544726 175044 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 403 5 1 5 3.2 Cc1c(C(=O)NCc2ccc(S(C)(=O)=O)cc2)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4565390 175044 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 403 5 1 5 3.2 Cc1c(C(=O)NCc2ccc(S(C)(=O)=O)cc2)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
44405194 71857 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 427 5 1 3 3.9 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H]2C[C@@H]1CN2Cc1ccc(F)cc1 10.1016/j.bmcl.2005.08.057
CHEMBL196908 71857 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 427 5 1 3 3.9 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H]2C[C@@H]1CN2Cc1ccc(F)cc1 10.1016/j.bmcl.2005.08.057
44405181 132892 None 0 Human Functional pIC50 = 5.8 5.8 51 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370162 132892 None 0 Human Functional pIC50 = 5.8 5.8 51 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
512282 758 None 42 Human Functional pIC50 = 7.8 7.8 141 5
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
767 758 None 42 Human Functional pIC50 = 7.8 7.8 141 5
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
CHEMBL232656 758 None 42 Human Functional pIC50 = 7.8 7.8 141 5
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
512282 758 None 42 Human Functional pIC50 = 7.8 7.8 141 5
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
767 758 None 42 Human Functional pIC50 = 7.8 7.8 141 5
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
CHEMBL232656 758 None 42 Human Functional pIC50 = 7.8 7.8 141 5
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
44430713 86750 None 0 Human Functional pIC50 = 7.8 7.8 30 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL231829 86750 None 0 Human Functional pIC50 = 7.8 7.8 30 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453467 95785 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL258359 95785 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453363 97579 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2007.09.068
CHEMBL270433 97579 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2007.09.068
44453501 97859 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL271903 97859 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453292 155569 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 448 4 1 4 3.8 Cc1ccccc1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404033 155569 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 448 4 1 4 3.8 Cc1ccccc1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
58138893 175590 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 466 7 2 5 3.8 CC(C)NS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4577460 175590 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 466 7 2 5 3.8 CC(C)NS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
11801020 12252 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 434 7 1 1 6.4 C[N+]1(CCCC(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL1184558 12252 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 434 7 1 1 6.4 C[N+]1(CCCC(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL356099 12252 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 434 7 1 1 6.4 C[N+]1(CCCC(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
22725647 173803 None 0 Human Functional pIC50 = 5.7 5.7 -52 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173803 None 0 Human Functional pIC50 = 5.7 5.7 -52 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
44430745 142138 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 544 11 2 8 3.0 COCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387822 142138 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 544 11 2 8 3.0 COCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
45138458 171791 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 6 1 7 2.7 CCS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4466500 171791 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 6 1 7 2.7 CCS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
44453164 95787 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1OC(F)(F)F 10.1016/j.bmcl.2007.09.068
CHEMBL258361 95787 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1OC(F)(F)F 10.1016/j.bmcl.2007.09.068
10001921 72477 None 0 Human Functional pIC50 = 6.7 6.7 3 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
CHEMBL198852 72477 None 0 Human Functional pIC50 = 6.7 6.7 3 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
155533145 171924 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 409 4 1 2 6.3 Cc1cc(-c2ccc(Cl)cc2)sc1C(=O)NCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2018.11.015
CHEMBL4468514 171924 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 409 4 1 2 6.3 Cc1cc(-c2ccc(Cl)cc2)sc1C(=O)NCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2018.11.015
10766998 34032 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 476 7 1 4 5.5 COc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1Br 10.1021/jm990316l
CHEMBL142468 34032 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 476 7 1 4 5.5 COc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1Br 10.1021/jm990316l
22725647 173803 None 0 Human Functional pIC50 = 5.7 5.7 -52 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173803 None 0 Human Functional pIC50 = 5.7 5.7 -52 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10164 874 None 26 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 4 1 8 2.2 COc1cc(ccc1Cl)N1CCN(CC1)C(=O)Cn1[nH]c(=C2N=CC=N2)c2c1nccc2 10.1016/j.bmcl.2018.11.015
135565361 874 None 26 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 4 1 8 2.2 COc1cc(ccc1Cl)N1CCN(CC1)C(=O)Cn1[nH]c(=C2N=CC=N2)c2c1nccc2 10.1016/j.bmcl.2018.11.015
CHEMBL4444976 874 None 26 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 4 1 8 2.2 COc1cc(ccc1Cl)N1CCN(CC1)C(=O)Cn1[nH]c(=C2N=CC=N2)c2c1nccc2 10.1016/j.bmcl.2018.11.015
52917500 172371 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 465 5 1 7 3.2 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CCC2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4474606 172371 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 465 5 1 7 3.2 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CCC2)ccn1 10.1016/j.bmcl.2018.12.024
59278436 172409 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 6 2 6 2.4 CNS(=O)(=O)c1ccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4475173 172409 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 439 6 2 6 2.4 CNS(=O)(=O)c1ccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
10049340 102698 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 448 11 3 5 3.3 CC(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL304358 102698 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 448 11 3 5 3.3 CC(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
512282 758 None 42 Human Functional pIC50 = 8.6 8.6 141 5
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
767 758 None 42 Human Functional pIC50 = 8.6 8.6 141 5
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
CHEMBL232656 758 None 42 Human Functional pIC50 = 8.6 8.6 141 5
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
44405181 132892 None 0 Human Functional pIC50 = 8.6 8.6 51 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370162 132892 None 0 Human Functional pIC50 = 8.6 8.6 51 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
49865951 16206 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 463 4 1 4 5.7 Cc1nnc([C@H]2CCCN2C(=O)Nc2ccc(C(F)(F)F)cc2)n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224189 16206 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 463 4 1 4 5.7 Cc1nnc([C@H]2CCCN2C(=O)Nc2ccc(C(F)(F)F)cc2)n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
10072252 72643 None 0 Human Functional pIC50 = 7.7 7.7 17 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL199412 72643 None 0 Human Functional pIC50 = 7.7 7.7 17 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
10434371 72982 None 0 Human Functional pIC50 = 7.7 7.7 5 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL200629 72982 None 0 Human Functional pIC50 = 7.7 7.7 5 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
11719164 140356 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 441 5 1 3 4.3 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL380568 140356 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 441 5 1 3 4.3 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
44453637 98042 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL272758 98042 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
6918497 113493 None 1 Mouse Functional pIC50 = 7.7 7.7 -17 4
inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptorinhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Functional pIC50 = 7.7 7.7 -17 4
inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptorinhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Functional pIC50 = 7.7 7.7 -17 4
inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptorinhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptor
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
44453229 95452 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL256889 95452 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2007.09.068
58138845 176227 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 429 4 1 3 5.6 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4591935 176227 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 429 4 1 3 5.6 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.12.024
155562877 175330 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 403 5 1 5 3.2 Cc1c(C(=O)NCc2cccc(S(C)(=O)=O)c2)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4571547 175330 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 403 5 1 5 3.2 Cc1c(C(=O)NCc2cccc(S(C)(=O)=O)c2)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
25254218 16192 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1ncnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224120 16192 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1ncnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
24782826 189695 None 4 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL514611 189695 None 4 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.082
25233755 179443 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 457 4 1 2 5.2 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1F 10.1021/jm801416q
CHEMBL473532 179443 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 457 4 1 2 5.2 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1F 10.1021/jm801416q
24782826 189695 None 4 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1021/jm801416q
CHEMBL514611 189695 None 4 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1021/jm801416q
58138826 170505 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4448064 170505 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
44309195 102203 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 496 9 3 5 3.6 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
CHEMBL302533 102203 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 496 9 3 5 3.6 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
44453167 95789 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL258363 95789 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
44453195 155266 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 496 4 1 4 4.8 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(C)(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL402327 155266 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 496 4 1 4 4.8 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(C)(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453197 155503 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.5 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403665 155503 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.5 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
44430748 87255 None 0 Human Functional pIC50 = 7.6 7.6 72 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232837 87255 None 0 Human Functional pIC50 = 7.6 7.6 72 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453504 95580 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1cccs1 10.1016/j.bmcl.2007.09.068
CHEMBL257452 95580 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1cccs1 10.1016/j.bmcl.2007.09.068
10003548 71996 None 0 Mouse Functional pIC50 = 4.6 4.6 -223 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197345 71996 None 0 Mouse Functional pIC50 = 4.6 4.6 -223 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@@H](C)N(Cc2ccc(F)cc2)C[C@@H]1C 10.1016/j.bmcl.2005.08.057
52916803 171085 None 20 Human Functional pIC50 = 7.6 7.6 - 1
Affinity Phenotypic Cellular interaction (Functional cellular assay (measuring calcium flux in response to MIP-1a in CCR1-transfected cells)) EUB0000352a CCR1Affinity Phenotypic Cellular interaction (Functional cellular assay (measuring calcium flux in response to MIP-1a in CCR1-transfected cells)) EUB0000352a CCR1
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL5209897
CHEMBL4456123 171085 None 20 Human Functional pIC50 = 7.6 7.6 - 1
Affinity Phenotypic Cellular interaction (Functional cellular assay (measuring calcium flux in response to MIP-1a in CCR1-transfected cells)) EUB0000352a CCR1Affinity Phenotypic Cellular interaction (Functional cellular assay (measuring calcium flux in response to MIP-1a in CCR1-transfected cells)) EUB0000352a CCR1
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL5209897
46858281 171511 None 3 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 394 4 1 4 4.2 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)nnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4462565 171511 None 3 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 394 4 1 4 4.2 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)nnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
44453433 160933 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.09.068
CHEMBL411476 160933 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.09.068
44430723 86875 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 544 8 2 7 3.1 CNc1c(Nc2cc(Br)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232253 86875 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 544 8 2 7 3.1 CNc1c(Nc2cc(Br)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44469380 170349 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccccc1F 10.1016/j.bmcl.2018.12.024
CHEMBL4445779 170349 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 413 4 1 3 5.1 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccccc1F 10.1016/j.bmcl.2018.12.024
9889700 118652 None 11 Human Functional pIC50 = 5.6 5.6 11 4
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL34166 118652 None 11 Human Functional pIC50 = 5.6 5.6 11 4
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
44453464 95354 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 488 4 1 4 3.9 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL256449 95354 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 488 4 1 4 3.9 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
58138911 174718 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 463 4 1 3 6.3 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4557554 174718 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 463 4 1 3 6.3 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2018.12.024
76336764 106243 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL 766 12 4 4 12.8 CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(O)c(C(=O)O)c5)c5cc(Cl)c(O)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138187 106243 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL 766 12 4 4 12.8 CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(O)c(C(=O)O)c5)c5cc(Cl)c(O)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138134 213579 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6ccccc6C(=O)O)c(C(=O)O)c5)c5cc(Cl)c(OCc6ccccc6C(=O)O)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138376 213579 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6ccccc6C(=O)O)c(C(=O)O)c5)c5cc(Cl)c(OCc6ccccc6C(=O)O)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
44453157 155357 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL402827 155357 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
155538947 172887 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 4 1 3 5.5 Cc1c(C(=O)N[C@@H](C)c2cccc(C(F)(F)F)c2F)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4513370 172887 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 4 1 3 5.5 Cc1c(C(=O)N[C@@H](C)c2cccc(C(F)(F)F)c2F)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
44405203 72511 None 0 Human Functional pIC50 = 7.6 7.6 31 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
CHEMBL198966 72511 None 0 Human Functional pIC50 = 7.6 7.6 31 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
44453161 95322 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.5 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL256271 95322 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.5 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
44453435 97654 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL270863 97654 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2007.09.068
44537841 675 None 16 Human Functional pIC50 = 8.5 8.5 114 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
57889181 675 None 16 Human Functional pIC50 = 8.5 8.5 114 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
9497 675 None 16 Human Functional pIC50 = 8.5 8.5 114 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
CHEMBL2398716 675 None 16 Human Functional pIC50 = 8.5 8.5 114 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
CHEMBL3334824 675 None 16 Human Functional pIC50 = 8.5 8.5 114 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
45138007 170556 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 414 4 1 4 4.5 O=C(NCc1cccc(C(F)(F)F)c1)c1cncc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4448761 170556 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 414 4 1 4 4.5 O=C(NCc1cccc(C(F)(F)F)c1)c1cncc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4638406 216504 None 5 Human Functional pIC50 = 8.5 8.5 - 1
CCR1 cellular Ca2+-flux assayCCR1 cellular Ca2+-flux assay
ChEMBL None None None CCOc1cc(N2C3COCC2CN(C(=O)[C@H]2C[C@H](O)CN2c2ccc(Cl)cc2)C3)ccc1Cl 10.6019/CHEMBL4630906
71462570 82598 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assayAntagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assay
ChEMBL 518 5 2 5 5.6 CC1(C)CN(CC/C=C2/c3cc(C(=O)O)ccc3OCc3ncccc32)C[C@H](c2ccc(Cl)cc2)[C@H]1O 10.1021/jm300682j
CHEMBL2178569 82598 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assayAntagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assay
ChEMBL 518 5 2 5 5.6 CC1(C)CN(CC/C=C2/c3cc(C(=O)O)ccc3OCc3ncccc32)C[C@H](c2ccc(Cl)cc2)[C@H]1O 10.1021/jm300682j
44453403 95189 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL255629 95189 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2007.09.068
44453202 95346 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 422 7 2 4 3.3 Cc1ccccc1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL256404 95346 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 422 7 2 4 3.3 Cc1ccccc1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
11743399 72508 None 9 Human Functional pIC50 = 7.5 7.5 32 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL198949 72508 None 9 Human Functional pIC50 = 7.5 7.5 32 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
10072252 72643 None 0 Human Functional pIC50 = 7.5 7.5 17 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL199412 72643 None 0 Human Functional pIC50 = 7.5 7.5 17 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
11554849 72877 None 0 Human Functional pIC50 = 7.5 7.5 2 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200242 72877 None 0 Human Functional pIC50 = 7.5 7.5 2 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
44405211 133662 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 441 5 1 3 4.3 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2005.08.057
CHEMBL371248 133662 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 441 5 1 3 4.3 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2005.08.057
9980155 71840 None 0 Mouse Functional pIC50 = 6.5 6.5 -23 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
CHEMBL196860 71840 None 0 Mouse Functional pIC50 = 6.5 6.5 -23 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
10072252 72643 None 0 Human Functional pIC50 = 6.5 6.5 17 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL199412 72643 None 0 Human Functional pIC50 = 6.5 6.5 17 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 446 5 1 4 4.1 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44405202 73019 None 0 Mouse Functional pIC50 = 5.5 5.5 -17 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
CHEMBL200794 73019 None 0 Mouse Functional pIC50 = 5.5 5.5 -17 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
44405181 132892 None 0 Mouse Functional pIC50 = 5.5 5.5 -51 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370162 132892 None 0 Mouse Functional pIC50 = 5.5 5.5 -51 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
9804868 33846 None 1 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 472 5 1 4 6.0 N#CC1(CCCN2CCC(O)(c3ccc(F)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL142318 33846 None 1 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 472 5 1 4 6.0 N#CC1(CCCN2CCC(O)(c3ccc(F)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
44309122 102875 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 482 11 4 6 3.4 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NO 10.1016/j.bmcl.2004.02.022
CHEMBL305423 102875 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 482 11 4 6 3.4 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NO 10.1016/j.bmcl.2004.02.022
1370410 86936 None 9 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assay
ChEMBL 404 3 0 4 3.4 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322888 86936 None 9 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assay
ChEMBL 404 3 0 4 3.4 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2013.01.005
11743399 72508 None 9 Human Functional pIC50 = 6.5 6.5 32 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL198949 72508 None 9 Human Functional pIC50 = 6.5 6.5 32 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
10811393 34895 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 407 7 1 4 4.8 N#CCC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL143194 34895 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 407 7 1 4 4.8 N#CCC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
44453227 95450 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 548 4 1 4 4.5 O=S(=O)(c1c(F)cc(F)cc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL256887 95450 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 548 4 1 4 4.5 O=S(=O)(c1c(F)cc(F)cc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10649043 34563 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 499 5 1 4 5.5 CN1C(=O)c2ccccc2C(C#N)(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1021/jm990316l
CHEMBL142925 34563 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 499 5 1 4 5.5 CN1C(=O)c2ccccc2C(C#N)(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1021/jm990316l
45138010 170962 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1ccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cn1 10.1016/j.bmcl.2018.12.024
CHEMBL4454067 170962 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1ccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)cn1 10.1016/j.bmcl.2018.12.024
25233754 179442 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 473 4 1 2 5.7 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1Cl 10.1021/jm801416q
CHEMBL473531 179442 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 473 4 1 2 5.7 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1Cl 10.1021/jm801416q
44453469 95786 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL258360 95786 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2007.09.068
155526212 171140 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 406 4 1 2 5.7 Cc1cc(C(=O)NCc2cccc(C(F)(F)F)c2)c(C)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4456839 171140 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 406 4 1 2 5.7 Cc1cc(C(=O)NCc2cccc(C(F)(F)F)c2)c(C)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
44453437 160934 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL411477 160934 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.068
44405180 140720 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 431 6 1 3 4.1 CC(=O)Nc1cc(Cl)ccc1CCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL381446 140720 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 431 6 1 3 4.1 CC(=O)Nc1cc(Cl)ccc1CCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44453165 95788 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL258362 95788 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
44453263 155731 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL404732 155731 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.068
44430755 153514 None 0 Human Functional pIC50 = 7.4 7.4 42 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL397910 153514 None 0 Human Functional pIC50 = 7.4 7.4 42 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453528 97593 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1016/j.bmcl.2007.09.068
CHEMBL270564 97593 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1016/j.bmcl.2007.09.068
44430753 142110 None 0 Human Functional pIC50 = 7.4 7.4 77 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387608 142110 None 0 Human Functional pIC50 = 7.4 7.4 77 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
25252974 16205 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nncn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224188 16205 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nncn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
17753030 87045 None 0 Human Functional pIC50 = 8.4 8.4 39 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232441 87045 None 0 Human Functional pIC50 = 8.4 8.4 39 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
10434371 72982 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL200629 72982 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
44405176 135476 None 0 Mouse Functional pIC50 = 8.4 8.4 -1 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL372807 135476 None 0 Mouse Functional pIC50 = 8.4 8.4 -1 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
58138789 172414 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 2 5 3.0 CNS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4475237 172414 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 2 5 3.0 CNS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
21070989 86923 None 0 Human Functional pIC50 = 8.3 8.3 354 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced calcium flux by FLIPR assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced calcium flux by FLIPR assay
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Functional pIC50 = 8.3 8.3 354 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced calcium flux by FLIPR assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced calcium flux by FLIPR assay
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44453291 97476 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL269957 97476 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
44453361 167419 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 456 7 2 4 4.0 Cc1cccc(Cl)c1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL429419 167419 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 456 7 2 4 4.0 Cc1cccc(Cl)c1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
512282 758 None 42 Human Functional pIC50 = 7.4 7.4 141 5
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
767 758 None 42 Human Functional pIC50 = 7.4 7.4 141 5
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
CHEMBL232656 758 None 42 Human Functional pIC50 = 7.4 7.4 141 5
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
11554849 72877 None 0 Mouse Functional pIC50 = 7.4 7.4 -2 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200242 72877 None 0 Mouse Functional pIC50 = 7.4 7.4 -2 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
9980155 71840 None 0 Human Functional pIC50 = 7.4 7.4 23 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
CHEMBL196860 71840 None 0 Human Functional pIC50 = 7.4 7.4 23 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
9845614 121346 None 19 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 430 6 1 3 5.5 N#CC(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL357919 121346 None 19 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 430 6 1 3 5.5 N#CC(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL3138115 213581 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6cccc(B(O)O)c6)c(C(=O)O)c5)c5cc(Cl)c(OCc6cccc(B(O)O)c6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138540 213581 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6cccc(B(O)O)c6)c(C(=O)O)c5)c5cc(Cl)c(OCc6cccc(B(O)O)c6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
59278474 172235 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 6 1 7 2.8 O=C(NCc1ccnc(S(=O)(=O)C2CC2)c1)c1cncc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4472994 172235 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 451 6 1 7 2.8 O=C(NCc1ccnc(S(=O)(=O)C2CC2)c1)c1cncc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
11554849 72877 None 0 Human Functional pIC50 = 7.4 7.4 2 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200242 72877 None 0 Human Functional pIC50 = 7.4 7.4 2 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
44453321 97543 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1c(Cl)cccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270254 97543 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1c(Cl)cccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
155561040 175477 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 418 6 2 5 2.7 CNS(=O)(=O)c1ccc(CNC(=O)c2cnn(-c3ccc(Cl)cc3)c2C)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4574870 175477 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 418 6 2 5 2.7 CNS(=O)(=O)c1ccc(CNC(=O)c2cnn(-c3ccc(Cl)cc3)c2C)cc1 10.1016/j.bmcl.2018.11.015
44453290 97475 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL269956 97475 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
59278286 171658 None 1 Mouse Functional pIC50 = 7.4 7.4 -112 2
Antagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4464625 171658 None 1 Mouse Functional pIC50 = 7.4 7.4 -112 2
Antagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
44469942 175050 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 452 6 1 5 3.3 CN(C)S(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4565496 175050 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 452 6 1 5 3.3 CN(C)S(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
25233582 190211 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 401 5 1 3 4.0 COc1ccc(NC(=O)N2CCC[C@@H]2C(=O)N(C)Cc2ccc(Cl)cc2)cc1 10.1021/jm801416q
CHEMBL517290 190211 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 401 5 1 3 4.0 COc1ccc(NC(=O)N2CCC[C@@H]2C(=O)N(C)Cc2ccc(Cl)cc2)cc1 10.1021/jm801416q
44309245 205902 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 556 13 3 5 5.2 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.02.022
CHEMBL65784 205902 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 556 13 3 5 5.2 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.02.022
10001921 72477 None 0 Mouse Functional pIC50 = 6.4 6.4 -3 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
CHEMBL198852 72477 None 0 Mouse Functional pIC50 = 6.4 6.4 -3 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
9980155 71840 None 0 Human Functional pIC50 = 7.4 7.4 23 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
CHEMBL196860 71840 None 0 Human Functional pIC50 = 7.4 7.4 23 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 430 5 2 3 3.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1NC(N)=O 10.1016/j.bmcl.2005.08.057
45138012 170312 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 414 4 1 4 4.5 O=C(NCc1cccc(C(F)(F)F)c1)c1nccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4445316 170312 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 414 4 1 4 4.5 O=C(NCc1cccc(C(F)(F)F)c1)c1nccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
58138781 175206 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 379 4 1 3 4.7 O=C(NCc1cccc(Cl)c1)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4568987 175206 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 379 4 1 3 4.7 O=C(NCc1cccc(Cl)c1)c1cccc2c1cnn2-c1ccc(F)cc1 10.1016/j.bmcl.2018.12.024
44453198 95670 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 516 4 1 4 5.2 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL257853 95670 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 516 4 1 4 5.2 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
44430746 87151 None 0 Human Functional pIC50 = 7.3 7.3 41 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232638 87151 None 0 Human Functional pIC50 = 7.3 7.3 41 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44480348 175882 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 446 7 1 6 3.9 CCCC(NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1ccc(S(C)(=O)=O)nc1 10.1016/j.bmcl.2018.11.015
CHEMBL4583870 175882 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 446 7 1 6 3.9 CCCC(NC(=O)c1cnn(-c2ccc(Cl)cc2)c1C)c1ccc(S(C)(=O)=O)nc1 10.1016/j.bmcl.2018.11.015
44453639 158956 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL409498 158956 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
44405203 72511 None 0 Mouse Functional pIC50 = 5.3 5.3 -31 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
CHEMBL198966 72511 None 0 Mouse Functional pIC50 = 5.3 5.3 -31 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 443 4 1 4 4.5 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)oc12 10.1016/j.bmcl.2005.08.057
10503785 121183 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 451 7 1 4 5.3 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)N1CCCCC1 10.1021/jm990316l
CHEMBL357434 121183 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 451 7 1 4 5.3 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)N1CCCCC1 10.1021/jm990316l
59687824 82601 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1Antagonist activity at CCR1
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1NC1CC[C@@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1021/jm300682j
CHEMBL2178572 82601 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1Antagonist activity at CCR1
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1NC1CC[C@@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1021/jm300682j
44430753 142110 None 0 Human Functional pIC50 = 8.3 8.3 77 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387608 142110 None 0 Human Functional pIC50 = 8.3 8.3 77 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44470083 171681 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 466 7 2 5 3.8 CC(C)NS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4465000 171681 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 466 7 2 5 3.8 CC(C)NS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
44309312 206236 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 460 9 3 5 3.4 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCCC1 10.1016/j.bmcl.2004.02.022
CHEMBL68145 206236 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 460 9 3 5 3.4 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCCC1 10.1016/j.bmcl.2004.02.022
21070989 86923 None 0 Human Functional pIC50 = 8.3 8.3 354 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assay
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Functional pIC50 = 8.3 8.3 354 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced calcium flux by FLIPR assay
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44453200 95721 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2007.09.068
CHEMBL258065 95721 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2007.09.068
44405181 132892 None 0 Human Functional pIC50 = 7.3 7.3 51 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370162 132892 None 0 Human Functional pIC50 = 7.3 7.3 51 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 432 6 2 4 3.6 CC(=O)Nc1cc(Cl)ccc1NCC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
10434371 72982 None 0 Mouse Functional pIC50 = 7.3 7.3 -5 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL200629 72982 None 0 Mouse Functional pIC50 = 7.3 7.3 -5 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
44405212 72993 None 0 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 458 5 1 4 4.2 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200680 72993 None 0 Mouse Functional pIC50 = 7.3 7.3 -1 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 458 5 1 4 4.2 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
155549724 173965 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 427 4 1 3 5.4 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2018.11.015
CHEMBL4539264 173965 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 427 4 1 3 5.4 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2018.11.015
10388824 133506 None 0 Mouse Functional pIC50 = 6.3 6.3 -4 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370596 133506 None 0 Mouse Functional pIC50 = 6.3 6.3 -4 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
9870185 84130 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR1Antagonist activity at CCR1
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2207666 84130 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR1Antagonist activity at CCR1
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
162658125 181202 None 0 Human Functional pIC50 = 5.3 5.3 -125 3
Antagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181202 None 0 Human Functional pIC50 = 5.3 5.3 -125 3
Antagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162666730 182380 None 1 Human Functional pIC50 = 5.3 5.3 -707 3
Antagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182380 None 1 Human Functional pIC50 = 5.3 5.3 -707 3
Antagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR1 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL3 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44453436 97700 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
CHEMBL271079 97700 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
44453293 167500 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 486 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
CHEMBL429591 167500 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 486 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
9869274 119377 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 468 5 1 3 6.4 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C=Cc2ccccc21 10.1021/jm990316l
CHEMBL344073 119377 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 468 5 1 3 6.4 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C=Cc2ccccc21 10.1021/jm990316l
44430745 142138 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 544 11 2 8 3.0 COCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387822 142138 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 544 11 2 8 3.0 COCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
10111333 175571 None 0 Human Functional pIC50 = 6.3 6.3 -19 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175571 None 0 Human Functional pIC50 = 6.3 6.3 -19 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
58138841 169739 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 2 5 3.0 CNS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4437170 169739 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 438 6 2 5 3.0 CNS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
512282 758 None 42 Human Functional pIC50 = 6.3 6.3 141 5
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
767 758 None 42 Human Functional pIC50 = 6.3 6.3 141 5
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
CHEMBL232656 758 None 42 Human Functional pIC50 = 6.3 6.3 141 5
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.08.057
44405202 73019 None 0 Human Functional pIC50 = 6.3 6.3 17 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
CHEMBL200794 73019 None 0 Human Functional pIC50 = 6.3 6.3 17 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
10576419 34207 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 472 9 1 3 6.7 N#CC(CCCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL142620 34207 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 472 9 1 3 6.7 N#CC(CCCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL3138380 213580 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6cccc([N+](=O)[O-])c6)c(C(=O)O)c5)c5cc(Cl)c(OCc6cccc([N+](=O)[O-])c6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138437 213580 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6cccc([N+](=O)[O-])c6)c(C(=O)O)c5)c5cc(Cl)c(OCc6cccc([N+](=O)[O-])c6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
10001921 72477 None 0 Human Functional pIC50 = 7.2 7.2 3 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
CHEMBL198852 72477 None 0 Human Functional pIC50 = 7.2 7.2 3 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 415 5 1 3 3.8 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.057
11743399 72508 None 9 Mouse Functional pIC50 = 6.2 6.2 -32 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL198949 72508 None 9 Mouse Functional pIC50 = 6.2 6.2 -32 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
10572669 119505 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 393 6 1 4 4.6 N#Cc1ccccc1C(C#N)CCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL344989 119505 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 393 6 1 4 4.6 N#Cc1ccccc1C(C#N)CCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
3497 1181 None 25 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1016/j.bmcl.2018.11.015
5311123 1181 None 25 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1016/j.bmcl.2018.11.015
CHEMBL1628706 1181 None 25 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1016/j.bmcl.2018.11.015
44453499 155493 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403613 155493 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10111333 175571 None 0 Human Functional pIC50 = 6.2 6.2 -19 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175571 None 0 Human Functional pIC50 = 6.2 6.2 -19 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
44430748 87255 None 0 Human Functional pIC50 = 8.2 8.2 72 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232837 87255 None 0 Human Functional pIC50 = 8.2 8.2 72 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44430758 142897 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 482 6 2 6 3.1 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL389293 142897 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 482 6 2 6 3.1 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
25233756 180988 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 467 4 1 2 5.6 Cc1cc(C(F)(F)F)cc(C)c1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL475748 180988 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrsAntagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
ChEMBL 467 4 1 2 5.6 Cc1cc(C(F)(F)F)cc(C)c1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
58138880 172455 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 452 6 1 5 3.3 CN(C)S(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4475918 172455 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 452 6 1 5 3.3 CN(C)S(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
44405212 72993 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 458 5 1 4 4.2 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200680 72993 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonistic activity at rat CCR1 in CHO-K1 cellsAntagonistic activity at rat CCR1 in CHO-K1 cells
ChEMBL 458 5 1 4 4.2 CC(=O)Nc1cc2ncccc2cc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
25253284 16191 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 450 4 1 5 4.8 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nnnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224119 16191 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrs
ChEMBL 450 4 1 5 4.8 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nnnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
59278314 170021 None 24 Human Functional pIC50 = 8.2 8.2 54 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4441094 170021 None 24 Human Functional pIC50 = 8.2 8.2 54 2
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
11211557 169957 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 393 4 1 3 4.8 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4440166 169957 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 393 4 1 3 4.8 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2018.11.015
10456104 72006 None 0 Mouse Functional pIC50 = 6.2 6.2 -56 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197375 72006 None 0 Mouse Functional pIC50 = 6.2 6.2 -56 2
Antagonistic activity at mouse CCR1 in CHO-K1 cellsAntagonistic activity at mouse CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
59278235 173188 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cncc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4519965 173188 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cncc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
44468708 174795 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 423 5 1 5 3.5 CS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4559388 174795 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 423 5 1 5 3.5 CS(=O)(=O)c1cccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
44453466 155739 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404757 155739 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453502 155233 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL402110 155233 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44309353 103459 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL308473 103459 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
44453226 95792 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 536 4 1 4 5.4 O=S(=O)(c1ccc(Cl)c(Cl)c1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL258369 95792 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 536 4 1 4 5.4 O=S(=O)(c1ccc(Cl)c(Cl)c1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
59278314 170021 None 24 Mouse Functional pIC50 = 6.2 6.2 -54 2
Antagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4441094 170021 None 24 Mouse Functional pIC50 = 6.2 6.2 -54 2
Antagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at mouse CCR1 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
44468570 171972 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 423 5 1 5 3.5 CS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
CHEMBL4469176 171972 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 423 5 1 5 3.5 CS(=O)(=O)c1ccc(CNC(=O)c2cccc3c2cnn3-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2018.12.024
44309219 102167 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 512 9 4 6 2.8 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
CHEMBL302320 102167 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 512 9 4 6 2.8 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
44309313 102582 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1ccccc1F)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL304053 102582 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1ccccc1F)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
10434371 72982 None 0 Human Functional pIC50 = 7.2 7.2 5 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL200629 72982 None 0 Human Functional pIC50 = 7.2 7.2 5 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 459 6 1 4 4.2 COc1cc(/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
17753030 87045 None 0 Human Functional pIC50 = 8.2 8.2 39 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232441 87045 None 0 Human Functional pIC50 = 8.2 8.2 39 2
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxisAntagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44405176 135476 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL372807 135476 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
44405176 135476 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
CHEMBL372807 135476 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 471 6 1 4 4.3 COc1cc(/C=C/C(=O)N2C3CCC2CN(Cc2ccc(F)cc2)C3)c(NC(C)=O)cc1Cl 10.1016/j.bmcl.2005.08.057
44453529 97893 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1016/j.bmcl.2007.09.068
CHEMBL272097 97893 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1016/j.bmcl.2007.09.068
10076510 11643 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 433 6 1 2 6.0 C[N+]1(CCCC(C#N)c2ccc3ccccc3c2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL1180795 11643 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 433 6 1 2 6.0 C[N+]1(CCCC(C#N)c2ccc3ccccc3c2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL143374 11643 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 433 6 1 2 6.0 C[N+]1(CCCC(C#N)c2ccc3ccccc3c2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
5311125 35181 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 488 5 1 4 6.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL143492 35181 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 488 5 1 4 6.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
10717972 119415 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 440 8 1 5 4.4 CCOC(=O)C(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL344324 119415 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 440 8 1 5 4.4 CCOC(=O)C(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
44309077 206786 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 549 11 2 6 3.6 CN1CCN(C(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2004.02.022
CHEMBL71499 206786 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 549 11 2 6 3.6 CN1CCN(C(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2004.02.022
10695080 12206 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 418 6 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1021/jm990316l
CHEMBL1184276 12206 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 418 6 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1021/jm990316l
CHEMBL342444 12206 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 418 6 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1021/jm990316l
44453163 155509 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 454 4 1 5 3.9 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2cccs2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403692 155509 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 454 4 1 5 3.9 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2cccs2)CC1 10.1016/j.bmcl.2007.09.068
44309124 206319 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 520 11 2 5 4.5 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)N1CCCC1 10.1016/j.bmcl.2004.02.022
CHEMBL68692 206319 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 520 11 2 5 4.5 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)N1CCCC1 10.1016/j.bmcl.2004.02.022
58138788 171259 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 395 4 1 3 5.0 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccccc1 10.1016/j.bmcl.2018.12.024
CHEMBL4458721 171259 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 395 4 1 3 5.0 O=C(NCc1cccc(C(F)(F)F)c1)c1cccc2c1cnn2-c1ccccc1 10.1016/j.bmcl.2018.12.024
9956488 119302 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 472 5 1 4 5.8 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2COc2ccccc21 10.1021/jm990316l
CHEMBL343511 119302 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 472 5 1 4 5.8 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2COc2ccccc21 10.1021/jm990316l
9956380 168352 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 470 5 1 3 6.0 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CCc2ccccc21 10.1021/jm990316l
CHEMBL433746 168352 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 470 5 1 3 6.0 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CCc2ccccc21 10.1021/jm990316l
24758044 82895 None 0 Human Functional pIC50 = 7.1 7.1 14 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis incubated for 60 mins at 37 degCAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis incubated for 60 mins at 37 degC
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180528 82895 None 0 Human Functional pIC50 = 7.1 7.1 14 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis incubated for 60 mins at 37 degCAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis incubated for 60 mins at 37 degC
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
37664972 170601 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 377 4 1 3 4.3 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(F)cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4449368 170601 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 377 4 1 3 4.3 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(F)cc1 10.1016/j.bmcl.2018.11.015
44453317 97499 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 480 5 1 5 4.2 CSc1ccc(C2(O)CCN(C3CCN(S(=O)(=O)c4ccccc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL270033 97499 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 480 5 1 5 4.2 CSc1ccc(C2(O)CCN(C3CCN(S(=O)(=O)c4ccccc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2007.09.068
44430755 153514 None 0 Human Functional pIC50 = 8.1 8.1 42 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL397910 153514 None 0 Human Functional pIC50 = 8.1 8.1 42 2
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPRAntagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
59278123 172450 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 424 5 1 6 2.9 CS(=O)(=O)c1cccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4475801 172450 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 424 5 1 6 2.9 CS(=O)(=O)c1cccc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)c1 10.1016/j.bmcl.2018.12.024
44309286 102389 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 512 9 4 6 3.7 O=C(N[C@@H](Cc1ccccc1)[C@@H](O)CC(C(=O)NO)C1CCC(F)(F)CC1)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
CHEMBL303673 102389 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 512 9 4 6 3.7 O=C(N[C@@H](Cc1ccccc1)[C@@H](O)CC(C(=O)NO)C1CCC(F)(F)CC1)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
44453228 95451 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1F 10.1016/j.bmcl.2007.09.068
CHEMBL256888 95451 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1F 10.1016/j.bmcl.2007.09.068
10388824 133506 None 0 Human Functional pIC50 = 7.1 7.1 4 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL370596 133506 None 0 Human Functional pIC50 = 7.1 7.1 4 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 445 5 1 3 4.7 CC(=O)Nc1cc2ccccc2cc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44405196 140657 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 460 5 2 4 3.8 COc1cc2c(cc1Cl)NC(=O)NC2CC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL381223 140657 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 460 5 2 4 3.8 COc1cc2c(cc1Cl)NC(=O)NC2CC(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44453641 97989 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 438 8 2 5 3.0 COc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL272559 97989 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 438 8 2 5 3.0 COc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
10789482 33693 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 444 9 1 3 5.9 N#CC(CCCCl)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL142191 33693 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 444 9 1 3 5.9 N#CC(CCCCl)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
44453584 97976 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 484 8 2 4 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.068
CHEMBL272523 97976 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 484 8 2 4 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.068
44308819 206356 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.022
CHEMBL68937 206356 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inhibition of CCL3 induced chemotaxis in human T lymphocytesInhibition of CCL3 induced chemotaxis in human T lymphocytes
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.022
10547456 119650 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1021/jm990316l
CHEMBL346205 119650 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1021/jm990316l
24758044 82895 None 0 Human Functional pIC50 = 7.1 7.1 14 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CK-8beta-induced calcium flux by FLIPRAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CK-8beta-induced calcium flux by FLIPR
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180528 82895 None 0 Human Functional pIC50 = 7.1 7.1 14 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CK-8beta-induced calcium flux by FLIPRAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CK-8beta-induced calcium flux by FLIPR
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
155514261 169939 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169939 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
155514261 169939 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169939 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
10526132 72502 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 419 7 1 2 6.2 OC1(c2ccc(Cl)cc2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
CHEMBL142004 72502 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 419 7 1 2 6.2 OC1(c2ccc(Cl)cc2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
CHEMBL198935 72502 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 419 7 1 2 6.2 OC1(c2ccc(Cl)cc2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
11554849 72877 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
CHEMBL200242 72877 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 484 7 1 4 3.9 CN(C)CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C2CCC1CN(Cc1ccc(F)cc1)C2 10.1016/j.bmcl.2005.08.057
10456104 72006 None 0 Human Functional pIC50 = 8.1 8.1 56 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL197375 72006 None 0 Human Functional pIC50 = 8.1 8.1 56 2
Antagonistic activity at human CCR1 in CHO-K1 cellsAntagonistic activity at human CCR1 in CHO-K1 cells
ChEMBL 443 5 1 3 4.6 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
3536 3906 None 0 Human Functional pIC50 = 8.0 8.0 9 2
Antagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assayAntagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assay
ChEMBL 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10.1021/jm300682j
44560289 3906 None 0 Human Functional pIC50 = 8.0 8.0 9 2
Antagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assayAntagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assay
ChEMBL 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10.1021/jm300682j
CHEMBL1186993 3906 None 0 Human Functional pIC50 = 8.0 8.0 9 2
Antagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assayAntagonist activity at CCR1 assessed as inhibition of CCL3-induced chemotaxis by cell based assay
ChEMBL 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10.1021/jm300682j
44405202 73019 None 0 Human Functional pIC50 = 8.0 8.0 17 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
CHEMBL200794 73019 None 0 Human Functional pIC50 = 8.0 8.0 17 2
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cellsAntagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
ChEMBL 442 4 2 3 4.3 CC(=O)Nc1cc(Cl)cc2cc(C(=O)N3CCN(Cc4ccc(F)cc4)C[C@H]3C)[nH]c12 10.1016/j.bmcl.2005.08.057
11743399 72508 None 9 Human Functional pIC50 = 8 8.0 32 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
CHEMBL198949 72508 None 9 Human Functional pIC50 = 8 8.0 32 2
Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1Inhibitory effect on transwell chemotaxis induced by 1 nM MIP-1alpha in mouse pre-B cells transfected with human CCR1
ChEMBL 429 5 1 3 4.2 CC(=O)Nc1cc(Cl)ccc1/C=C/C(=O)N1CCN(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2005.08.057
44453359 97613 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 408 7 2 4 3.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/j.bmcl.2007.09.068
CHEMBL270631 97613 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 408 7 2 4 3.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/j.bmcl.2007.09.068
25022507 155515 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403728 155515 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assayAntagonist activity at human CCR1 receptor expressed in THP1 cells assessed as human MIP-1-alpha-stimulated intracellular calcium level by FLIPR assay
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10833944 118820 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(O)c1 10.1021/jm990316l
CHEMBL341840 118820 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(O)c1 10.1021/jm990316l
CHEMBL3138118 213577 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6ccc(-c7cccc(C(=O)O)c7)cc6)c(C(=O)O)c5)c5cc(Cl)c(OCc6ccc(-c7cccc(C(=O)O)c7)cc6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
CHEMBL3138133 213577 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectantsInhibition of RANTES-induced migration of human embryonic kidney (CCR1/HEK) cell transfectants
ChEMBL None None None CC(C)CCCC(C)[C@H]1CC[C@H]2[C@@H]3CCC4C[C@@H](CCC=C(c5cc(Cl)c(OCc6ccc(-c7cccc(C(=O)O)c7)cc6)c(C(=O)O)c5)c5cc(Cl)c(OCc6ccc(-c7cccc(C(=O)O)c7)cc6)c(C(=O)O)c5)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/s0960-894x(00)00601-6
155521447 170687 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170687 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
155521447 170687 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170687 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
Antagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL3-induced G-protein activation preincubated for 30 mins in presence of CCL3 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
155549273 173939 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 404 5 1 5 4.0 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc([N+](=O)[O-])cc1 10.1016/j.bmcl.2018.11.015
CHEMBL4538794 173939 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assayAntagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
ChEMBL 404 5 1 5 4.0 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc([N+](=O)[O-])cc1 10.1016/j.bmcl.2018.11.015
10690854 32756 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1021/jm990316l
CHEMBL141387 32756 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptorInhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1021/jm990316l
49798289 10653 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10653 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798265 10732 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10732 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
10300214 84233 None 0 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at CCR1Antagonist activity at CCR1
ChEMBL 492 9 2 5 5.0 O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208416 84233 None 0 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at CCR1Antagonist activity at CCR1
ChEMBL 492 9 2 5 5.0 O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1 10.1016/j.bmcl.2012.09.113
49798264 10791 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10791 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
19430534 10776 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10776 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrsAntagonist activity at human CCR1 assessed as inhibition of MIP-1-alpha-induced [35S]-GTPgammaS binding after 3 to 4 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
15664 83821 None 63 Human Functional pEC50 = 8.3 8.3 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 83821 None 63 Human Functional pEC50 = 8.3 8.3 -3 3
Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis
Drug Central 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 None
3536 3906 None 0 Human Functional pIC50 = 8.0 8.0 9 2
Measuring antagonism of CCL3-induced chemotaxis <i>in vitro</i>.Measuring antagonism of CCL3-induced chemotaxis <i>in vitro</i>.
Guide to Pharmacology 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10854442
44560289 3906 None 0 Human Functional pIC50 = 8.0 8.0 9 2
Measuring antagonism of CCL3-induced chemotaxis <i>in vitro</i>.Measuring antagonism of CCL3-induced chemotaxis <i>in vitro</i>.
Guide to Pharmacology 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10854442
CHEMBL1186993 3906 None 0 Human Functional pIC50 = 8.0 8.0 9 2
Measuring antagonism of CCL3-induced chemotaxis <i>in vitro</i>.Measuring antagonism of CCL3-induced chemotaxis <i>in vitro</i>.
Guide to Pharmacology 515 5 1 2 7.3 CC[N+]1(CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2c1cc(Cl)cc2)CC1CCCCCC1 10854442
4382 833 None 0 Human Functional pIC50 = 6.1 6.1 -25 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23951310
754 830 None 0 Human Functional pIC50 = 7.9 7.9 -5 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
126523866 1056 None 0 Human Functional pIC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 584 6 2 5 6.0 NC[C@@H]1CCCN(C1)C(=O)c1ccc2c(c1)C(C(=O)NC1CCN(CC1)CC1=CCCCCCCC1)c1c(O2)cccc1 12614873
3696 1056 None 0 Human Functional pIC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 584 6 2 5 6.0 NC[C@@H]1CCCN(C1)C(=O)c1ccc2c(c1)C(C(=O)NC1CCN(CC1)CC1=CCCCCCCC1)c1c(O2)cccc1 12614873
73755059 1056 None 0 Human Functional pIC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 584 6 2 5 6.0 NC[C@@H]1CCCN(C1)C(=O)c1ccc2c(c1)C(C(=O)NC1CCN(CC1)CC1=CCCCCCCC1)c1c(O2)cccc1 12614873
10750 2579 None 0 Human Functional pIC50 = 9.1 9.1 5011 2
UnclassifiedUnclassified
Guide to Pharmacology 532 5 2 5 6.3 Clc1ccc(cc1)C1(O)CCN(CC1(C)C)CC/C=C\1/c2cc(ccc2OCc2c1cccn2)C(O)(C)C None
18437138 2579 None 0 Human Functional pIC50 = 9.1 9.1 5011 2
UnclassifiedUnclassified
Guide to Pharmacology 532 5 2 5 6.3 Clc1ccc(cc1)C1(O)CCN(CC1(C)C)CC/C=C\1/c2cc(ccc2OCc2c1cccn2)C(O)(C)C None
486830 4002 None 0 Human Functional pIC50 None 8.1 8.1 -10 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217
768 4002 None 0 Human Functional pIC50 None 8.1 8.1 -10 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
72548703 161661 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161661 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
25109291 191495 None 6 Human Binding pIC50 = 10.1 10.1 56 12
Displacement of radiolabeled MIP1alpha from human CCR1 receptorDisplacement of radiolabeled MIP1alpha from human CCR1 receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 191495 None 6 Human Binding pIC50 = 10.1 10.1 56 12
Displacement of radiolabeled MIP1alpha from human CCR1 receptorDisplacement of radiolabeled MIP1alpha from human CCR1 receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
59278286 171658 None 1 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4464625 171658 None 1 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
11744314 87388 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 446 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2332935 87388 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 446 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
68959963 87386 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 432 6 2 5 3.1 CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332933 87386 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 432 6 2 5 3.1 CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
11744314 87388 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 446 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332935 87388 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 446 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
10094212 87389 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 430 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2332936 87389 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 430 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.04.047
10094212 87389 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 430 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332936 87389 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 430 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
72945512 104381 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 471 7 4 6 3.0 O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)NC1CC1 10.1016/j.bmcl.2013.11.062
CHEMBL3099947 104381 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 471 7 4 6 3.0 O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)NC1CC1 10.1016/j.bmcl.2013.11.062
10478859 87384 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 448 6 2 5 3.6 CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332931 87384 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 448 6 2 5 3.6 CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
25141109 130348 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 493 5 4 4 3.8 C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O nan
CHEMBL3679659 130348 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 493 5 4 4 3.8 C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O nan
25141109 130348 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 493 5 4 4 3.8 C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O nan
CHEMBL3679659 130348 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 493 5 4 4 3.8 C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O nan
71570633 87393 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 445 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332940 87393 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 445 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
21070989 86923 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889003 91189 None 5 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888919 91192 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398729 91192 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
72945510 104379 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 487 7 4 6 3.5 O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)NC1CC1 10.1016/j.bmcl.2013.11.062
CHEMBL3099945 104379 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 487 7 4 6 3.5 O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)NC1CC1 10.1016/j.bmcl.2013.11.062
6918497 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards C-C chemokine receptor type 1Binding affinity towards C-C chemokine receptor type 1
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(03)00748-0
CHEMBL277930 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards C-C chemokine receptor type 1Binding affinity towards C-C chemokine receptor type 1
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(03)00748-0
CHEMBL331897 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards C-C chemokine receptor type 1Binding affinity towards C-C chemokine receptor type 1
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(03)00748-0
6918497 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL277930 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL331897 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(01)00176-7
10389562 87383 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 460 7 2 6 3.5 COc1ccc(NC(C)=O)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2012.12.095
CHEMBL2332930 87383 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 460 7 2 6 3.5 COc1ccc(NC(C)=O)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2012.12.095
6918497 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Human Binding pIC50 = 9.1 9.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
10032207 90819 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 536 6 3 7 3.1 O=C(c1cc(Cl)c(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391803 90819 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 536 6 3 7 3.1 O=C(c1cc(Cl)c(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
9954423 87385 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 430 6 2 5 3.5 CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332932 87385 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 430 6 2 5 3.5 CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
10409538 87387 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 414 6 2 5 3.0 CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332934 87387 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 414 6 2 5 3.0 CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
57889003 91189 None 5 Human Binding pIC50 = 9 9.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of RANTES-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of RANTES-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 9 9.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of RANTES-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of RANTES-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889327 91180 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 420 6 2 3 3.7 CC(C)[C@@H](NC(=O)CC1CC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398717 91180 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 420 6 2 3 3.7 CC(C)[C@@H](NC(=O)CC1CC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
25175119 130340 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 533 5 3 5 3.0 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(S(N)(=O)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679651 130340 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 533 5 3 5 3.0 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(S(N)(=O)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
44537841 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57888993 114539 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 471 6 3 3 4.3 CC(C)[C@@H](NC(=O)NCc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334818 114539 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 471 6 3 3 4.3 CC(C)[C@@H](NC(=O)NCc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
59278286 171658 None 1 Human Binding pIC50 = 9 9.0 - 0
Inhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysisInhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysis
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
CHEMBL4464625 171658 None 1 Human Binding pIC50 = 9 9.0 - 0
Inhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysisInhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysis
ChEMBL 453 6 1 7 3.2 CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 10.1016/j.bmcl.2018.12.024
25175119 130340 None 0 Human Binding pIC50 = 9 9.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 533 5 3 5 3.0 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(S(N)(=O)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679651 130340 None 0 Human Binding pIC50 = 9 9.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 533 5 3 5 3.0 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(S(N)(=O)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
68963686 90826 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 516 6 3 7 2.9 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCC(O)CC1 10.1016/j.bmcl.2013.04.047
CHEMBL2391810 90826 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 516 6 3 7 2.9 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCC(O)CC1 10.1016/j.bmcl.2013.04.047
512282 758 None 42 Human Binding pIC50 = 9.0 9.0 147 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2018.11.015
767 758 None 42 Human Binding pIC50 = 9.0 9.0 147 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2018.11.015
CHEMBL232656 758 None 42 Human Binding pIC50 = 9.0 9.0 147 2
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2018.11.015
57889430 91191 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398728 91191 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888834 91207 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 436 7 2 3 4.4 CC(C)CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398744 91207 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 436 7 2 3 4.4 CC(C)CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
57889764 91229 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 457 6 2 4 3.6 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398769 91229 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 457 6 2 4 3.6 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
6918497 113493 None 1 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL277930 113493 None 1 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL331897 113493 None 1 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1016/j.ejmech.2020.113085
6918497 113493 None 1 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
71655299 90813 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 529 7 2 7 3.0 CN(C)[C@@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391797 90813 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 529 7 2 7 3.0 CN(C)[C@@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
25175289 130344 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 446 4 2 3 4.3 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)C2CCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679655 130344 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 446 4 2 3 4.3 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)C2CCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
72945311 104376 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 461 6 4 6 3.0 CNC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099942 104376 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 461 6 4 6 3.0 CNC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
25175289 130344 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 446 4 2 3 4.3 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)C2CCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679655 130344 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 446 4 2 3 4.3 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)C2CCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
10367570 90811 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 472 7 3 6 3.1 O=C(NC1CC1)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391795 90811 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 472 7 3 6 3.1 O=C(NC1CC1)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
10412648 90850 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 474 7 2 5 3.6 O=C(NC1CC1)c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391939 90850 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 474 7 2 5 3.6 O=C(NC1CC1)c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
57889423 91210 None 0 Human Binding pIC50 = 8.9 8.9 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 434 5 2 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398747 91210 None 0 Human Binding pIC50 = 8.9 8.9 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 434 5 2 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
68959770 104374 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 485 6 2 5 4.2 O=C(Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCCC1 10.1016/j.bmcl.2013.11.062
CHEMBL3099940 104374 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 485 6 2 5 4.2 O=C(Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCCC1 10.1016/j.bmcl.2013.11.062
42602331 87394 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 429 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332941 87394 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 429 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
21070989 86923 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL15/Leukotactin1-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44537841 675 None 16 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
57889181 675 None 16 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
9497 675 None 16 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2018.11.015
25141158 176348 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 471 5 2 4 4.4 Cc1cc(C)c(C(=O)NC(C)(C)CC(=O)N2CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C2)cn1 nan
CHEMBL4436541 176348 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 471 5 2 4 4.4 Cc1cc(C)c(C(=O)NC(C)(C)CC(=O)N2CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C2)cn1 nan
CHEMBL4594791 176348 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 471 5 2 4 4.4 Cc1cc(C)c(C(=O)NC(C)(C)CC(=O)N2CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C2)cn1 nan
25175123 130342 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@H]2CC[C@@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679653 130342 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@H]2CC[C@@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25175123 130342 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@H]2CC[C@@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679653 130342 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@H]2CC[C@@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
57889430 91191 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398728 91191 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
25175288 130343 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 498 5 3 4 4.1 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(=O)O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679654 130343 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 498 5 3 4 4.1 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(=O)O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25175288 130343 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 498 5 3 4 4.1 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(=O)O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679654 130343 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 498 5 3 4 4.1 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(=O)O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
57889230 91202 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 484 8 2 3 5.0 CC(C)[C@@H](NC(=O)CCCc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398739 91202 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 484 8 2 3 5.0 CC(C)[C@@H](NC(=O)CCCc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888834 91207 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 436 7 2 3 4.4 CC(C)CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398744 91207 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 436 7 2 3 4.4 CC(C)CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
25206951 175442 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 434 5 2 3 4.3 CC(C)(CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)C1CCCC1 nan
CHEMBL4574123 175442 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 434 5 2 3 4.3 CC(C)(CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)C1CCCC1 nan
42602328 90809 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 446 6 3 6 2.6 CNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391793 90809 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 446 6 3 6 2.6 CNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
10368175 90824 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 486 6 2 6 3.5 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCCC1 10.1016/j.bmcl.2013.04.047
CHEMBL2391808 90824 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 486 6 2 6 3.5 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCCC1 10.1016/j.bmcl.2013.04.047
66686405 175343 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 532 5 2 5 6.3 CC(C)(O)c1ccc2c(c1)/C(=C\CCN1CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C1)c1cccnc1CO2 10.1016/j.bmcl.2018.11.015
CHEMBL4571977 175343 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 532 5 2 5 6.3 CC(C)(O)c1ccc2c(c1)/C(=C\CCN1CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C1)c1cccnc1CO2 10.1016/j.bmcl.2018.11.015
57889897 91200 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 456 6 2 3 4.2 CC(C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398737 91200 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 456 6 2 3 4.2 CC(C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889071 91209 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 420 5 2 3 3.7 CC(C)[C@@H](NC(=O)C1CCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398746 91209 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 420 5 2 3 3.7 CC(C)[C@@H](NC(=O)C1CCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
59444283 172488 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 485 6 3 4 3.5 CC(C)(CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)c1cccc(C(N)=O)c1 nan
CHEMBL4476397 172488 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 485 6 3 4 3.5 CC(C)(CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)c1cccc(C(N)=O)c1 nan
59474992 130345 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 497 5 3 4 3.5 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(N)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679656 130345 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 497 5 3 4 3.5 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(N)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
72945313 104377 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 521 7 4 6 4.2 O=C(Nc1cc(Cl)c(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)NC1CC1 10.1016/j.bmcl.2013.11.062
CHEMBL3099943 104377 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 521 7 4 6 4.2 O=C(Nc1cc(Cl)c(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)NC1CC1 10.1016/j.bmcl.2013.11.062
72945314 104378 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 501 8 3 6 3.8 COc1ccc(NC(=O)NC2CC2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2013.11.062
CHEMBL3099944 104378 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 501 8 3 6 3.8 COc1ccc(NC(=O)NC2CC2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2013.11.062
59474992 130345 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 497 5 3 4 3.5 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(N)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679656 130345 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 497 5 3 4 3.5 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)c2cccc(C(N)=O)c2)CC[C@]1(O)c1ccc(Cl)cc1 nan
10436125 90820 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 502 6 3 7 2.5 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391804 90820 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 502 6 3 7 2.5 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
57889334 91206 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 422 6 2 3 4.0 CC(C)CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398743 91206 None 0 Human Binding pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 422 6 2 3 4.0 CC(C)CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
59444225 171779 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 467 6 4 4 3.4 C[C@H](NC(=O)NC(C)(C)CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O nan
CHEMBL4466344 171779 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 467 6 4 4 3.4 C[C@H](NC(=O)NC(C)(C)CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O nan
11803142 12018 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 615 5 1 2 7.8 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1183314 12018 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 615 5 1 2 7.8 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL289902 12018 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 615 5 1 2 7.8 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
57889736 114534 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334727 114534 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57889679 91221 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 442 5 2 3 4.2 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398761 91221 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 442 5 2 3 4.2 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888966 91231 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1cccc(Cl)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398771 91231 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1cccc(Cl)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889613 91222 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 432 5 2 3 4.3 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398762 91222 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 432 5 2 3 4.3 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
57840192 86831 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 460 5 0 7 2.3 COc1cc(N2CCN(C(=O)Cn3nc(S(C)(=O)=O)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2321887 86831 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 460 5 0 7 2.3 COc1cc(N2CCN(C(=O)Cn3nc(S(C)(=O)=O)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57840295 86893 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 407 4 0 6 2.7 COc1cc(N2CCN(C(=O)Cn3nc(C#N)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322847 86893 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 407 4 0 6 2.7 COc1cc(N2CCN(C(=O)Cn3nc(C#N)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57840511 86915 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 466 5 1 6 3.1 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CO)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322867 86915 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 466 5 1 6 3.1 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CO)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
71719855 86928 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 484 4 0 5 4.5 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(Cl)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322880 86928 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 484 4 0 5 4.5 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(Cl)c1Cl 10.1016/j.bmcl.2013.01.005
17753030 87045 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232441 87045 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
59278314 170021 None 24 Human Binding pIC50 = 8 8.0 - 0
Inhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysisInhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysis
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4441094 170021 None 24 Human Binding pIC50 = 8 8.0 - 0
Inhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysisInhibition of MIP1alpha-stimulated CCR1 internalization in human whole blood preincubated for 30 mins followed by MIP1alpha-stimulation and measured after 40 mins by Alexa647 staining based FACS analysis
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
512282 758 None 42 Human Binding pIC50 = 8 8.0 147 2
Inhibition of human recombinant CCR1Inhibition of human recombinant CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/acs.jmedchem.6b01309
767 758 None 42 Human Binding pIC50 = 8 8.0 147 2
Inhibition of human recombinant CCR1Inhibition of human recombinant CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/acs.jmedchem.6b01309
CHEMBL232656 758 None 42 Human Binding pIC50 = 8 8.0 147 2
Inhibition of human recombinant CCR1Inhibition of human recombinant CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/acs.jmedchem.6b01309
512282 758 None 42 Human Binding pIC50 = 8 8.0 147 2
Inhibition of human wild type CCR1Inhibition of human wild type CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/acs.jmedchem.6b01309
767 758 None 42 Human Binding pIC50 = 8 8.0 147 2
Inhibition of human wild type CCR1Inhibition of human wild type CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/acs.jmedchem.6b01309
CHEMBL232656 758 None 42 Human Binding pIC50 = 8 8.0 147 2
Inhibition of human wild type CCR1Inhibition of human wild type CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/acs.jmedchem.6b01309
21070993 86922 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 434 3 0 4 4.2 Cc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322874 86922 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 434 3 0 4 4.2 Cc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57888715 82878 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 5 1 2 5.1 Cc1cccc(C(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)c1C 10.1021/jm300896d
CHEMBL2180511 82878 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 5 1 2 5.1 Cc1cccc(C(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)c1C 10.1021/jm300896d
44430755 153514 None 0 Mouse Binding pIC50 = 6 6.0 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL397910 153514 None 0 Mouse Binding pIC50 = 6 6.0 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453527 97592 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 477 4 0 4 4.7 N#CC1(c2ccc(Cl)cc2)CCN(C2CCN(S(=O)(=O)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270563 97592 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 477 4 0 4 4.7 N#CC1(c2ccc(Cl)cc2)CCN(C2CCN(S(=O)(=O)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.09.068
5481702 208281 None 0 Human Binding pIC50 = 5 5.0 - 0
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR1 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR1 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 208281 None 0 Human Binding pIC50 = 5 5.0 - 0
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR1 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR1 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
11329244 71140 None 6 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 1Inhibition of C-C chemokine receptor type 1
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71140 None 6 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 1Inhibition of C-C chemokine receptor type 1
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11272103 124442 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 1Inhibition of C-C chemokine receptor type 1
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124442 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 1Inhibition of C-C chemokine receptor type 1
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
14338 4369 None 74 Human Binding pIC50 = 4 4.0 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
CHEMBL101165 4369 None 74 Human Binding pIC50 = 4 4.0 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
72792 202179 None 52 Human Binding pIC50 = 4 4.0 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 202179 None 52 Human Binding pIC50 = 4 4.0 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
44309060 103044 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 446 10 3 3 4.3 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.02.021
CHEMBL306683 103044 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 446 10 3 3 4.3 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.02.021
57889664 82832 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 7 1 2 5.1 Cc1ccc(CCC(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)cc1 10.1021/jm300896d
CHEMBL2180194 82832 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 7 1 2 5.1 Cc1ccc(CCC(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)cc1 10.1021/jm300896d
25175449 130329 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 526 4 2 5 4.1 CC1(C)CN(C(=O)[C@H]2CC3(CC[C@H]2NC(=O)c2ccccc2)OCCO3)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679640 130329 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 526 4 2 5 4.1 CC1(C)CN(C(=O)[C@H]2CC3(CC[C@H]2NC(=O)c2ccccc2)OCCO3)CC[C@]1(O)c1ccc(Cl)cc1 nan
25175449 130329 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 526 4 2 5 4.1 CC1(C)CN(C(=O)[C@H]2CC3(CC[C@H]2NC(=O)c2ccccc2)OCCO3)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679640 130329 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 526 4 2 5 4.1 CC1(C)CN(C(=O)[C@H]2CC3(CC[C@H]2NC(=O)c2ccccc2)OCCO3)CC[C@]1(O)c1ccc(Cl)cc1 nan
57888707 91228 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 413 6 1 3 3.8 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398768 91228 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 413 6 1 3 3.8 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
71718646 86926 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322878 86926 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C)c1Cl 10.1016/j.bmcl.2013.01.005
57888718 82885 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 428 6 1 3 5.0 CC(C)C(NC(=O)OCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180518 82885 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 428 6 1 3 5.0 CC(C)C(NC(=O)OCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
71719253 86901 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 480 5 1 6 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)[C@H](CO)C2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322854 86901 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 480 5 1 6 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)[C@H](CO)C2)ccc1Cl 10.1016/j.bmcl.2013.01.005
25233756 180988 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 467 4 1 2 5.6 Cc1cc(C(F)(F)F)cc(C)c1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL475748 180988 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 467 4 1 2 5.6 Cc1cc(C(F)(F)F)cc(C)c1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
118714034 114541 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 424 6 3 4 2.7 CC(C)[C@@H](NC(=O)C[C@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334820 114541 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 424 6 3 4 2.7 CC(C)[C@@H](NC(=O)C[C@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
68496383 170163 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 503 5 3 5 3.7 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2cccc(C(=O)O)c2)CC[C@]1(O)c1ccc(C#N)cc1 nan
CHEMBL4443024 170163 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 503 5 3 5 3.7 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2cccc(C(=O)O)c2)CC[C@]1(O)c1ccc(C#N)cc1 nan
59474993 130346 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 503 5 3 4 4.4 [C-]#[N+]c1ccc([C@@]2(O)CCN(C(=O)[C@H]3CCCC[C@H]3NC(=O)c3cccc(C(=O)O)c3)CC2(C)C)cc1 nan
CHEMBL3679657 130346 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 503 5 3 4 4.4 [C-]#[N+]c1ccc([C@@]2(O)CCN(C(=O)[C@H]3CCCC[C@H]3NC(=O)c3cccc(C(=O)O)c3)CC2(C)C)cc1 nan
25175448 130327 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 469 4 3 3 4.8 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679639 130327 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 469 4 3 3 4.8 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25175448 130327 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 469 4 3 3 4.8 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679639 130327 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 469 4 3 3 4.8 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
71655559 90821 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 529 7 2 7 3.0 CN(C)[C@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391805 90821 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 529 7 2 7 3.0 CN(C)[C@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
44453291 97476 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL269957 97476 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
21071070 86913 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 478 5 0 5 4.7 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C(C)C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322865 86913 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 478 5 0 5 4.7 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C(C)C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
10811980 100003 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 418 6 1 2 5.8 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(c1ccccc1)c1ccccc1 10.1021/jm0004244
CHEMBL286355 100003 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 418 6 1 2 5.8 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(c1ccccc1)c1ccccc1 10.1021/jm0004244
21071081 86921 None 1 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 420 3 0 4 3.9 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322873 86921 None 1 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 420 3 0 4 3.9 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2013.01.005
44453227 95450 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 548 4 1 4 4.5 O=S(=O)(c1c(F)cc(F)cc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL256887 95450 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 548 4 1 4 4.5 O=S(=O)(c1c(F)cc(F)cc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
57888832 82826 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 446 6 1 2 5.1 CC(C)[C@@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180188 82826 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 446 6 1 2 5.1 CC(C)[C@@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453436 97700 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
CHEMBL271079 97700 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
44453525 97556 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 452 4 1 4 3.6 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270358 97556 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 452 4 1 4 3.6 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
24758046 82874 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 5 1 2 4.6 CC(C)[C@@H](NC(=O)c1ccc(F)cc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180507 82874 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 5 1 2 4.6 CC(C)[C@@H](NC(=O)c1ccc(F)cc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
12015739 103671 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 413 10 3 4 3.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC(C)C)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
CHEMBL308690 103671 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 413 10 3 4 3.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC(C)C)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
59444213 171402 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 484 5 2 4 4.2 CC1(C)CN(C(=O)CC2(NC(=O)c3ccccc3)CCOCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL4460796 171402 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 484 5 2 4 4.2 CC1(C)CN(C(=O)CC2(NC(=O)c3ccccc3)CCOCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
59444196 175400 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 442 5 2 3 4.2 CC(NC(=O)c1ccccc1)C(C)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL4573109 175400 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 442 5 2 3 4.2 CC(NC(=O)c1ccccc1)C(C)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
68963562 90818 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 488 6 2 6 2.4 O=C(c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391802 90818 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 488 6 2 6 2.4 O=C(c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
10073725 90828 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 476 8 4 7 2.0 O=C(NCCO)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391812 90828 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 476 8 4 7 2.0 O=C(NCCO)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
57889974 91190 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398727 91190 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
21070989 86923 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL15/Leukotactin1 from CCR1 in human THP1 cellsDisplacement of [125I]-CCL15/Leukotactin1 from CCR1 in human THP1 cells
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL15/Leukotactin1 from CCR1 in human THP1 cellsDisplacement of [125I]-CCL15/Leukotactin1 from CCR1 in human THP1 cells
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
21070983 86924 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 5 0 5 4.3 CCOc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322876 86924 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 5 0 5 4.3 CCOc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
71718022 86934 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 480 5 1 6 3.4 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(CO)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322886 86934 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 480 5 1 6 3.4 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(CO)c1Cl 10.1016/j.bmcl.2013.01.005
44430752 88031 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234295 88031 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
11803142 12018 None 0 Mouse Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 615 5 1 2 7.8 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1183314 12018 None 0 Mouse Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 615 5 1 2 7.8 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL289902 12018 None 0 Mouse Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 615 5 1 2 7.8 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
6918497 113493 None 1 Mouse Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
25175446 130326 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 450 3 2 4 4.5 CC(C)(C)OC(=O)N[C@@H]1CCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL3679638 130326 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 450 3 2 4 4.5 CC(C)(C)OC(=O)N[C@@H]1CCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
25175446 130326 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 450 3 2 4 4.5 CC(C)(C)OC(=O)N[C@@H]1CCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL3679638 130326 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 450 3 2 4 4.5 CC(C)(C)OC(=O)N[C@@H]1CCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
71560163 86897 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 411 5 1 6 2.3 COc1cc(N2CCN(C(=O)Cn3nc(CN)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322850 86897 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 411 5 1 6 2.3 COc1cc(N2CCN(C(=O)Cn3nc(CN)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57840312 86919 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 382 4 0 5 2.9 COc1cc(N2CCN(C(=O)Cn3ncc(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322871 86919 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 382 4 0 5 2.9 COc1cc(N2CCN(C(=O)Cn3ncc(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
25233754 179442 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 473 4 1 2 5.7 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1Cl 10.1021/jm801416q
CHEMBL473531 179442 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 473 4 1 2 5.7 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1Cl 10.1021/jm801416q
57889591 82905 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 6 1 2 4.6 CCCC(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180538 82905 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 6 1 2 4.6 CCCC(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
155549724 173965 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 427 4 1 3 5.4 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2018.11.015
CHEMBL4539264 173965 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 427 4 1 3 5.4 Cc1c(C(=O)NCc2cccc(C(F)(F)F)c2)cnn1-c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2018.11.015
24758630 82861 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 5 1 2 5.4 O=C(N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C1CCCCC1)c1ccccc1 10.1021/jm300896d
CHEMBL2180494 82861 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 5 1 2 5.4 O=C(N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C1CCCCC1)c1ccccc1 10.1021/jm300896d
57889696 82894 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 384 5 1 2 4.3 CC[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180527 82894 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 384 5 1 2 4.3 CC[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57888938 91226 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 477 6 2 4 3.1 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398766 91226 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 477 6 2 4 3.1 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
11124782 118533 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 587 11 3 3 7.3 O=C(NCC1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL341306 118533 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 587 11 3 3 7.3 O=C(NCC1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44453357 97576 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 434 4 1 4 3.5 O=S(=O)(c1ccccc1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270419 97576 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 434 4 1 4 3.5 O=S(=O)(c1ccccc1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
57889164 91223 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 3 4 4.1 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398763 91223 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 3 4 4.1 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44431529 88022 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 490 9 1 5 4.0 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2C(=O)CCC(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL234263 88022 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 490 9 1 5 4.0 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2C(=O)CCC(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
57889660 91203 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 380 4 2 3 2.9 CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398740 91203 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 380 4 2 3 2.9 CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
21070989 86923 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL15/Leukotactin1 from CCR1 in human monocytesDisplacement of [125I]-CCL15/Leukotactin1 from CCR1 in human monocytes
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL15/Leukotactin1 from CCR1 in human monocytesDisplacement of [125I]-CCL15/Leukotactin1 from CCR1 in human monocytes
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
24758296 82824 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 430 6 1 2 4.6 CC(C)[C@@H](NC(=O)Cc1ccccc1F)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180186 82824 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 430 6 1 2 4.6 CC(C)[C@@H](NC(=O)Cc1ccccc1F)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
72945111 104394 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 459 7 3 6 2.8 CNC(=O)Nc1ccc(OC)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099960 104394 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 459 7 3 6 2.8 CNC(=O)Nc1ccc(OC)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
68958915 90817 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 470 6 2 6 2.2 O=C(c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1ccccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391801 90817 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 470 6 2 6 2.2 O=C(c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1ccccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
57888652 82906 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.9 CC(C)CC(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180539 82906 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.9 CC(C)CC(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44309267 206512 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL69978 206512 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccc2ccccc2n1 10.1016/j.bmcl.2004.02.021
25231480 190184 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 389 4 1 2 4.1 CN(Cc1ccc(F)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL517261 190184 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 389 4 1 2 4.1 CN(Cc1ccc(F)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
72947880 104390 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 445 5 2 7 3.7 Nc1nc2c(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)cccc2s1 10.1016/j.bmcl.2013.11.062
CHEMBL3099956 104390 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 445 5 2 7 3.7 Nc1nc2c(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)cccc2s1 10.1016/j.bmcl.2013.11.062
69437067 104391 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 444 5 1 6 4.5 Cc1nc2c(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)cccc2s1 10.1016/j.bmcl.2013.11.062
CHEMBL3099957 104391 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 444 5 1 6 4.5 Cc1nc2c(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)cccc2s1 10.1016/j.bmcl.2013.11.062
10628025 11177 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 523 6 1 2 7.6 O=C(NC1CC[N+](Cc2ccccc2)(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL1178588 11177 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 523 6 1 2 7.6 O=C(NC1CC[N+](Cc2ccccc2)(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL33586 11177 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 523 6 1 2 7.6 O=C(NC1CC[N+](Cc2ccccc2)(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
44453464 95354 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 488 4 1 4 3.9 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL256449 95354 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 488 4 1 4 3.9 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
11082578 118134 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 603 10 3 3 7.5 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cc(F)ccc1F 10.1021/jm0201767
CHEMBL340491 118134 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 603 10 3 3 7.5 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cc(F)ccc1F 10.1021/jm0201767
71719254 86929 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 528 4 0 5 4.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(Br)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322881 86929 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 528 4 0 5 4.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(Br)c1Cl 10.1016/j.bmcl.2013.01.005
25175122 130341 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@@H]2CC[C@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679652 130341 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@@H]2CC[C@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
24758297 82875 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 434 5 1 2 4.8 CC(C)[C@@H](NC(=O)c1ccc(F)c(F)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180508 82875 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 434 5 1 2 4.8 CC(C)[C@@H](NC(=O)c1ccc(F)c(F)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
10769447 11183 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL1178601 11183 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL34165 11183 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
10769447 11183 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178601 11183 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL34165 11183 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
25175122 130341 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@@H]2CC[C@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679652 130341 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 462 4 3 4 3.2 CC1(C)CN(C(=O)[C@H]2CCC[C@H]2NC(=O)[C@@H]2CC[C@H](O)C2)CC[C@]1(O)c1ccc(Cl)cc1 nan
44537841 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
25174956 130339 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 465 5 4 4 3.0 C[C@@H](O)CNC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL3679650 130339 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 465 5 4 4 3.0 C[C@@H](O)CNC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
25174956 130339 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 465 5 4 4 3.0 C[C@@H](O)CNC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL3679650 130339 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 465 5 4 4 3.0 C[C@@H](O)CNC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
24782826 189695 None 4 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL514611 189695 None 4 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.082
24782826 189695 None 4 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1021/jm801416q
CHEMBL514611 189695 None 4 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1021/jm801416q
57889255 82827 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 6 1 2 4.7 Cc1ccc(CC(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)cc1 10.1021/jm300896d
CHEMBL2180189 82827 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 6 1 2 4.7 Cc1ccc(CC(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)cc1 10.1021/jm300896d
44430726 87048 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 502 8 2 7 2.6 CNc1c(Nc2cc(F)c(F)cc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232455 87048 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 502 8 2 7 2.6 CNc1c(Nc2cc(F)c(F)cc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453293 167500 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 486 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
CHEMBL429591 167500 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 486 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
10765199 112890 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 432 4 1 3 5.9 O=C(NC1CCN(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1016/j.ejmech.2020.113085
CHEMBL33074 112890 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 432 4 1 3 5.9 O=C(NC1CCN(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1016/j.ejmech.2020.113085
10765199 112890 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 432 4 1 3 5.9 O=C(NC1CCN(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL33074 112890 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 432 4 1 3 5.9 O=C(NC1CCN(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
10676520 11176 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 617 5 1 2 7.9 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1178581 11176 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 617 5 1 2 7.9 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL33340 11176 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 617 5 1 2 7.9 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
10509339 12374 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 631 6 1 2 8.3 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1185511 12374 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 631 6 1 2 8.3 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL418589 12374 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 631 6 1 2 8.3 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
44453614 155355 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL402825 155355 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
11814253 117019 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cccc(C(F)(F)F)c1 10.1021/jm0201767
CHEMBL338624 117019 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1cccc(C(F)(F)F)c1 10.1021/jm0201767
71455572 82890 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 1 2 4.5 CC(C)[C@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180523 82890 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 1 2 4.5 CC(C)[C@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
21070989 86923 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at CCR1 in human monocytes assessed as inhibition of CCL15/Leukotactin1-induced chemotaxisAntagonist activity at CCR1 in human monocytes assessed as inhibition of CCL15/Leukotactin1-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at CCR1 in human monocytes assessed as inhibition of CCL15/Leukotactin1-induced chemotaxisAntagonist activity at CCR1 in human monocytes assessed as inhibition of CCL15/Leukotactin1-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889660 91203 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 380 4 2 3 2.9 CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398740 91203 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 380 4 2 3 2.9 CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
57889158 91197 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1ccccn1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398734 91197 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1ccccn1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44430754 166771 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2ccccn2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL428193 166771 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2ccccn2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44309165 206465 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 490 9 3 6 3.0 CC1CC([C@H](C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)C(N)=O)CC(C)O1 10.1016/j.bmcl.2004.02.021
CHEMBL69659 206465 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 490 9 3 6 3.0 CC1CC([C@H](C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)C(N)=O)CC(C)O1 10.1016/j.bmcl.2004.02.021
25174462 130335 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 496 6 2 3 5.1 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679646 130335 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 496 6 2 3 5.1 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174462 130335 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 496 6 2 3 5.1 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679646 130335 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 496 6 2 3 5.1 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
44453202 95346 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 422 7 2 4 3.3 Cc1ccccc1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL256404 95346 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 422 7 2 4 3.3 Cc1ccccc1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
10555351 116222 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 586 4 1 3 7.3 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Br)ccc2Oc2ccc(Br)cc21 10.1021/jm0004244
CHEMBL33580 116222 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 586 4 1 3 7.3 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Br)ccc2Oc2ccc(Br)cc21 10.1021/jm0004244
44309155 206493 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@@H](CC(C)C)C[C@@H](O)[C@@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
CHEMBL69822 206493 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@@H](CC(C)C)C[C@@H](O)[C@@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
24758743 82891 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 364 6 1 2 4.0 CC[C@@H](NC(=O)CC(C)C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180524 82891 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 364 6 1 2 4.0 CC[C@@H](NC(=O)CC(C)C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57888775 82908 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 5.0 CCCC(NC(=O)c1ccccc1C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180541 82908 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 5.0 CCCC(NC(=O)c1ccccc1C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57889484 91224 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 532 7 3 3 5.7 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398764 91224 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 532 7 3 3 5.7 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
11351191 86891 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 5 1 6 3.1 COc1cc(N2CCN(C(=O)Cn3nc(C(C)(C)O)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322845 86891 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 5 1 6 3.1 COc1cc(N2CCN(C(=O)Cn3nc(C(C)(C)O)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
71718023 86935 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 479 5 1 6 3.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(CN)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322887 86935 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 479 5 1 6 3.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(CN)c1Cl 10.1016/j.bmcl.2013.01.005
44537841 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
69437029 104389 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 427 5 1 5 4.6 Cc1cc2c(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)cccc2o1 10.1016/j.bmcl.2013.11.062
CHEMBL3099955 104389 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 427 5 1 5 4.6 Cc1cc2c(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)cccc2o1 10.1016/j.bmcl.2013.11.062
44430742 142137 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 557 11 2 8 2.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN(C)C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387821 142137 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 557 11 2 8 2.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN(C)C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44430724 152109 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 484 8 2 7 2.5 CNc1c(Nc2cc(F)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL396700 152109 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 484 8 2 7 2.5 CNc1c(Nc2cc(F)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453529 97893 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1016/j.bmcl.2007.09.068
CHEMBL272097 97893 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1016/j.bmcl.2007.09.068
44309347 206732 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 516 10 3 5 4.4 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL71242 206732 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 516 10 3 5 4.4 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
10502989 113386 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 434 6 2 3 4.9 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(O)(c1ccccc1)c1ccccc1 10.1021/jm0004244
CHEMBL33159 113386 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 434 6 2 3 4.9 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(O)(c1ccccc1)c1ccccc1 10.1021/jm0004244
57991685 91183 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](N)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398720 91183 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](N)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10875472 113723 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 568 10 3 4 6.6 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccncc1 10.1021/jm0201767
CHEMBL332277 113723 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 568 10 3 4 6.6 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccncc1 10.1021/jm0201767
44430753 142110 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387608 142110 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44309237 102874 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 463 10 4 5 3.4 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cc2ccccc2nc1O 10.1016/j.bmcl.2004.02.021
CHEMBL305420 102874 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 463 10 4 5 3.4 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cc2ccccc2nc1O 10.1016/j.bmcl.2004.02.021
71681400 91188 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@H]1N)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398725 91188 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@H]1N)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
25252974 16205 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nncn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224188 16205 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nncn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
10580015 11181 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 515 4 1 2 7.3 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL1178597 11181 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 515 4 1 2 7.3 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL33929 11181 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 515 4 1 2 7.3 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
25175450 130330 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 482 4 2 4 4.0 CC1(C)CN(C(=O)[C@H]2CC(=O)CC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679641 130330 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 482 4 2 4 4.0 CC1(C)CN(C(=O)[C@H]2CC(=O)CC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25175450 130330 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 482 4 2 4 4.0 CC1(C)CN(C(=O)[C@H]2CC(=O)CC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679641 130330 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 482 4 2 4 4.0 CC1(C)CN(C(=O)[C@H]2CC(=O)CC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
44430735 87983 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 528 10 2 7 3.8 CCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234081 87983 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 528 10 2 7 3.8 CCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
57889667 82898 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 458 5 2 3 3.7 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Br)cc2)CC1 10.1021/jm300896d
CHEMBL2180531 82898 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 458 5 2 3 3.7 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Br)cc2)CC1 10.1021/jm300896d
71452035 82879 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 5 1 2 5.1 Cc1cccc(C)c1C(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180512 82879 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 5 1 2 5.1 Cc1cccc(C)c1C(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
44430752 88031 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234295 88031 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 599 11 2 9 2.7 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCOCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
24738063 91218 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 419 5 1 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CCN(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398758 91218 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 419 5 1 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CCN(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889679 91221 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 442 5 2 3 4.2 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398761 91221 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 442 5 2 3 4.2 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57840356 86911 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 436 4 0 5 3.6 COc1cc(N2CCN(C(=O)Cn3cc(Cl)c(C(F)(F)F)n3)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322863 86911 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 436 4 0 5 3.6 COc1cc(N2CCN(C(=O)Cn3cc(Cl)c(C(F)(F)F)n3)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889975 82830 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 444 7 1 2 5.0 CC(C)[C@@H](NC(=O)CCc1ccccc1F)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180192 82830 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 444 7 1 2 5.0 CC(C)[C@@H](NC(=O)CCc1ccccc1F)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
24758298 82833 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 455 5 1 4 5.1 CC(C)[C@@H](NC(=O)c1nc2ccccc2s1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180195 82833 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 455 5 1 4 5.1 CC(C)[C@@H](NC(=O)c1nc2ccccc2s1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
71570634 87395 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 411 6 3 6 2.5 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1ccccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332942 87395 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 411 6 3 6 2.5 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1ccccc1O2 10.1016/j.bmcl.2012.12.095
44430748 87255 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232837 87255 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
25176235 130331 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 483 4 3 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679642 130331 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 483 4 3 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25176235 130331 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 483 4 3 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679642 130331 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 483 4 3 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)Nc2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174305 130333 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 470 4 2 5 3.6 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2cncnc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679644 130333 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 470 4 2 5 3.6 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2cncnc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174305 130333 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 470 4 2 5 3.6 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2cncnc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679644 130333 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 470 4 2 5 3.6 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2cncnc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
57889141 82888 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 427 6 2 2 4.6 CC(C)[C@@H](NC(=O)NCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180521 82888 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 427 6 2 2 4.6 CC(C)[C@@H](NC(=O)NCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57889796 82915 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 414 5 2 3 3.6 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180548 82915 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 414 5 2 3 3.6 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
73349030 91214 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398751 91214 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10555068 12014 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 443 4 1 1 6.7 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)c2c3ccccc3cc3ccccc23)CC1 10.1021/jm0004244
CHEMBL1183306 12014 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 443 4 1 1 6.7 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)c2c3ccccc3cc3ccccc23)CC1 10.1021/jm0004244
CHEMBL289682 12014 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 443 4 1 1 6.7 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)c2c3ccccc3cc3ccccc23)CC1 10.1021/jm0004244
21070982 86939 None 1 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 3 0 4 4.0 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322891 86939 None 1 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 3 0 4 4.0 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2013.01.005
57889592 82899 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 396 5 1 2 4.4 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CC=C(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180532 82899 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 396 5 1 2 4.4 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CC=C(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453433 160933 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.09.068
CHEMBL411476 160933 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.09.068
44309087 102450 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccnc2ccccc12 10.1016/j.bmcl.2004.02.021
CHEMBL303947 102450 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccnc2ccccc12 10.1016/j.bmcl.2004.02.021
57889180 114533 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334726 114533 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57840556 86904 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 4 0 5 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)cc3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322857 86904 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 4 0 5 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)cc3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
24758299 82828 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 7 1 2 5.1 Cc1ccccc1CCC(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180190 82828 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 7 1 2 5.1 Cc1ccccc1CCC(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
795 574 None 5 Human Binding pIC50 = 5.7 5.7 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
796 574 None 5 Human Binding pIC50 = 5.7 5.7 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
9913085 574 None 5 Human Binding pIC50 = 5.7 5.7 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
CHEMBL20921 574 None 5 Human Binding pIC50 = 5.7 5.7 - 1
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 480 6 2 6 5.1 O=C(NC1CCN(CC1)Cc1ccc(c(c1)Cl)Cl)CSc1nc2c(s1)cc(cc2)N 10.1016/s0960-894x(01)00176-7
44453637 98042 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL272758 98042 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
10505512 116626 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 498 4 1 3 7.1 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1021/jm0004244
CHEMBL33639 116626 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 498 4 1 3 7.1 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1021/jm0004244
57889625 82912 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 448 6 1 2 5.8 CCCC(NC(=O)c1ccc2ccccc2c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180545 82912 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 448 6 1 2 5.8 CCCC(NC(=O)c1ccc2ccccc2c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57888746 91184 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@@H](N)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398721 91184 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@@H](N)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
73347500 91216 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 475 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@](N)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398753 91216 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 475 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@](N)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44453638 166577 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL427834 166577 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
52916803 171085 None 20 Human Binding pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.1016/j.bmcl.2018.12.024
57888907 114538 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 437 6 3 3 3.9 CC[C@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
CHEMBL3334817 114538 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 437 6 3 3 3.9 CC[C@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
11744314 87388 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 446 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332935 87388 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 446 6 3 6 3.2 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2012.12.095
57840363 86900 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)[C@@H](C)C2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322853 86900 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)[C@@H](C)C2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889099 114532 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 449 5 3 3 4.1 CC(C)[C@@H](NC(=O)NC1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334725 114532 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 449 5 3 3 4.1 CC(C)[C@@H](NC(=O)NC1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
118714001 114535 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334728 114535 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57888907 114538 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 437 6 3 3 3.9 CC[C@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
CHEMBL3334817 114538 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 437 6 3 3 3.9 CC[C@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
118714035 114542 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334821 114542 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
118714036 114543 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 424 6 3 4 2.7 CC(C)[C@@H](NC(=O)C[C@@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334822 114543 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 424 6 3 4 2.7 CC(C)[C@@H](NC(=O)C[C@@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
118714037 114544 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334823 114544 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
118714038 114545 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 452 7 3 4 3.5 CC(C)[C@@H](NC(=O)CCC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334825 114545 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 452 7 3 4 3.5 CC(C)[C@@H](NC(=O)CCC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
10698568 11184 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL1178613 11184 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL34732 11184 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
10698568 11184 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178613 11184 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL34732 11184 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
57889003 91189 None 5 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
25175283 130325 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 468 4 2 3 4.8 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679637 130325 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 468 4 2 3 4.8 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25175283 130325 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 468 4 2 3 4.8 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679637 130325 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 468 4 2 3 4.8 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
71681399 91187 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1N)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398724 91187 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1N)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889077 91211 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 448 5 2 3 4.5 CC(C)[C@@H](NC(=O)C1CCCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398748 91211 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 448 5 2 3 4.5 CC(C)[C@@H](NC(=O)C1CCCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
59444189 172293 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 510 6 2 7 3.4 CC(C)(CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)c1cccc(-n2cnnn2)c1 nan
CHEMBL4473668 172293 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 510 6 2 7 3.4 CC(C)(CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)c1cccc(-n2cnnn2)c1 nan
72945511 104380 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 485 8 3 6 3.3 COc1ccc(NC(=O)NC2CC2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(F)ccc2O3)c1 10.1016/j.bmcl.2013.11.062
CHEMBL3099946 104380 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 485 8 3 6 3.3 COc1ccc(NC(=O)NC2CC2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(F)ccc2O3)c1 10.1016/j.bmcl.2013.11.062
57991707 91185 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398722 91185 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
71680936 91213 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 563 8 3 6 3.2 CC(C)[C@@H](NC(=O)C1CCCC1(O)CCN1CCOCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398750 91213 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 563 8 3 6 3.2 CC(C)[C@@H](NC(=O)C1CCCC1(O)CCN1CCOCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
52916803 171085 None 20 Human Binding pIC50 = 8.6 8.6 - 1
Affinity On-target Cellular interaction (Chemotaxis in THP-1 cells) EUB0000352a CCR1Affinity On-target Cellular interaction (Chemotaxis in THP-1 cells) EUB0000352a CCR1
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL5210121
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 8.6 8.6 - 1
Affinity On-target Cellular interaction (Chemotaxis in THP-1 cells) EUB0000352a CCR1Affinity On-target Cellular interaction (Chemotaxis in THP-1 cells) EUB0000352a CCR1
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL5210121
52916803 171085 None 20 Human Binding pIC50 = 8.6 8.6 - 1
ChemotaxisChemotaxis
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 8.6 8.6 - 1
ChemotaxisChemotaxis
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
21070989 86923 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL23/CKbeta8.1-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL23/CKbeta8.1-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL23/CKbeta8.1-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL23/CKbeta8.1-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
68963393 90816 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 504 6 2 6 2.9 O=C(c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391800 90816 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 504 6 2 6 2.9 O=C(c1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 10.1016/j.bmcl.2013.04.047
10480588 90849 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 486 8 2 6 3.5 COc1ccc(C(=O)NC2CC2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2013.04.047
CHEMBL2391938 90849 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 486 8 2 6 3.5 COc1ccc(C(=O)NC2CC2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2013.04.047
57889423 91210 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 434 5 2 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398747 91210 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 434 5 2 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10555108 11171 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 445 4 1 2 5.9 C[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178543 11171 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 445 4 1 2 5.9 C[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL32257 11171 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 445 4 1 2 5.9 C[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
10094212 87389 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 430 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332936 87389 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 430 6 3 6 2.7 CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2012.12.095
57889347 91212 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 514 6 2 3 5.5 CC(C)[C@@H](NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398749 91212 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 514 6 2 3 5.5 CC(C)[C@@H](NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889003 91189 None 5 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at human CCR1 assessed as inhibition of MPIF-1-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MPIF-1-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at human CCR1 assessed as inhibition of MPIF-1-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MPIF-1-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10072781 90848 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 456 7 2 5 3.4 O=C(NC1CC1)c1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391937 90848 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 456 7 2 5 3.4 O=C(NC1CC1)c1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
10531632 11173 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 473 6 1 2 6.7 CCC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178571 11173 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 473 6 1 2 6.7 CCC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL33050 11173 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 473 6 1 2 6.7 CCC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
57888919 91192 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398729 91192 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889334 91206 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 422 6 2 3 4.0 CC(C)CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398743 91206 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 422 6 2 3 4.0 CC(C)CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
57889164 91223 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 3 4 4.1 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398763 91223 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 3 4 4.1 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
71681244 91186 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@H]1O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398723 91186 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@H]1O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57840282 86892 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 460 4 0 5 3.6 COc1cc(N2CCN(C(=O)Cn3nc(Br)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322846 86892 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 460 4 0 5 3.6 COc1cc(N2CCN(C(=O)Cn3nc(Br)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
25253284 16191 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 450 4 1 5 4.8 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nnnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224119 16191 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 450 4 1 5 4.8 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1nnnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
24758406 82871 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 404 6 1 2 4.8 CC(C)[C@@H](NC(=O)CC1CCCC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180504 82871 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 404 6 1 2 4.8 CC(C)[C@@H](NC(=O)CC1CCCC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57889047 114531 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 457 5 3 3 4.6 CC(C)[C@@H](NC(=O)Nc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334724 114531 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 457 5 3 3 4.6 CC(C)[C@@H](NC(=O)Nc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
44430746 87151 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232638 87151 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44309195 102203 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 496 9 3 5 3.6 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
CHEMBL302533 102203 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 496 9 3 5 3.6 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
44430721 144605 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 502 8 2 7 3.1 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL390707 144605 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 502 8 2 7 3.1 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453320 97542 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270253 97542 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10525291 118139 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 404 4 1 3 5.1 O=C(NC1CCN(CC2CCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1016/j.ejmech.2020.113085
CHEMBL34053 118139 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 404 4 1 3 5.1 O=C(NC1CCN(CC2CCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1016/j.ejmech.2020.113085
10525291 118139 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 404 4 1 3 5.1 O=C(NC1CCN(CC2CCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL34053 118139 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 404 4 1 3 5.1 O=C(NC1CCN(CC2CCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
57991713 91219 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 502 5 2 3 5.4 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)C2(CCCC2)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398759 91219 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 502 5 2 3 5.4 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)C2(CCCC2)C1 10.1016/j.bmcl.2013.04.079
73350585 91181 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 441 5 2 4 3.4 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C2(CC2)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398718 91181 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 441 5 2 4 3.4 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C2(CC2)C1 10.1016/j.bmcl.2013.04.079
71719255 86932 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 507 5 1 6 3.2 CNC(=O)c1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(OC)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322884 86932 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 507 5 1 6 3.2 CNC(=O)c1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(OC)c1Cl 10.1016/j.bmcl.2013.01.005
10531239 12410 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 449 6 2 2 5.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0004244
CHEMBL1185795 12410 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 449 6 2 2 5.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0004244
CHEMBL433232 12410 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 449 6 2 2 5.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0004244
10769447 11183 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178601 11183 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL34165 11183 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 447 4 1 2 6.0 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
118714038 114545 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 452 7 3 4 3.5 CC(C)[C@@H](NC(=O)CCC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334825 114545 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 452 7 3 4 3.5 CC(C)[C@@H](NC(=O)CCC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
24758408 82829 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 7 1 2 5.1 Cc1cccc(CCC(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)c1 10.1021/jm300896d
CHEMBL2180191 82829 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 7 1 2 5.1 Cc1cccc(CCC(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)c1 10.1021/jm300896d
44309163 102770 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 11 3 5 3.5 CNC(=O)[C@H](CCC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL304845 102770 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 11 3 5 3.5 CNC(=O)[C@H](CCC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
71718647 86933 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 521 5 0 6 3.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C(=O)N(C)C)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322885 86933 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 521 5 0 6 3.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C(=O)N(C)C)c1Cl 10.1016/j.bmcl.2013.01.005
44430836 88026 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 522 8 2 8 3.5 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Cl)s3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234276 88026 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 522 8 2 8 3.5 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Cl)s3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453162 95323 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 526 4 1 4 4.6 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
CHEMBL256272 95323 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 526 4 1 4 4.6 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2007.09.068
71682816 91220 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 428 6 2 3 4.7 CC(C)[C@H](CN1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)c1ccccc1 10.1016/j.bmcl.2013.04.079
CHEMBL2398760 91220 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 428 6 2 3 4.7 CC(C)[C@H](CN1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)c1ccccc1 10.1016/j.bmcl.2013.04.079
44308819 206356 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.022
CHEMBL68937 206356 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.022
24745662 167744 None 2 Human Binding pIC50 = 7.6 7.6 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 484 7 1 5 3.4 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2CS(=O)(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
9935062 167744 None 2 Human Binding pIC50 = 7.6 7.6 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 484 7 1 5 3.4 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2CS(=O)(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL430166 167744 None 2 Human Binding pIC50 = 7.6 7.6 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 484 7 1 5 3.4 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2CS(=O)(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
57840512 86903 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)C[C@@H]2C)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322856 86903 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)C[C@@H]2C)ccc1Cl 10.1016/j.bmcl.2013.01.005
25233755 179443 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 457 4 1 2 5.2 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1F 10.1021/jm801416q
CHEMBL473532 179443 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 457 4 1 2 5.2 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C(F)(F)F)cc1F 10.1021/jm801416q
44308819 206356 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
44308819 206356 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.021
CHEMBL68937 206356 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
CHEMBL68937 206356 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.021
44309124 206319 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 520 11 2 5 4.5 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)N1CCCC1 10.1016/j.bmcl.2004.02.022
CHEMBL68692 206319 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 520 11 2 5 4.5 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)N1CCCC1 10.1016/j.bmcl.2004.02.022
57888663 91194 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 521 6 3 5 2.9 CC(C)[C@@H](NC(=O)c1ccc(S(N)(=O)=O)cc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398731 91194 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 521 6 3 5 2.9 CC(C)[C@@H](NC(=O)c1ccc(S(N)(=O)=O)cc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44430718 86795 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccccc3F)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232044 86795 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccccc3F)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
52916803 171085 None 20 Human Binding pIC50 = 7.6 7.6 - 1
Ca fluxCa flux
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 7.6 7.6 - 1
Ca fluxCa flux
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
24758174 82873 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 5 1 2 4.6 CC(C)[C@@H](NC(=O)c1cccc(F)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180506 82873 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 5 1 2 4.6 CC(C)[C@@H](NC(=O)c1cccc(F)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453504 95580 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1cccs1 10.1016/j.bmcl.2007.09.068
CHEMBL257452 95580 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1cccs1 10.1016/j.bmcl.2007.09.068
10505512 116626 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 498 4 1 3 7.1 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1021/jm0004244
CHEMBL33639 116626 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 498 4 1 3 7.1 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1021/jm0004244
10652533 11175 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 603 4 1 2 7.5 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1178579 11175 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 603 4 1 2 7.5 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL33223 11175 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 603 4 1 2 7.5 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
10995329 18188 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 563 13 4 4 5.5 O=C(NCCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL126978 18188 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 563 13 4 4 5.5 O=C(NCCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44308997 206197 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccc2ncccc2c1 10.1016/j.bmcl.2004.02.021
CHEMBL67803 206197 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1ccc2ncccc2c1 10.1016/j.bmcl.2004.02.021
44537841 675 None 16 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
24758176 82877 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 2 4.8 Cc1ccc(C(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)cc1 10.1021/jm300896d
CHEMBL2180510 82877 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 2 4.8 Cc1ccc(C(=O)N[C@@H](C(=O)N2CCC(c3ccc(Cl)cc3)CC2)C(C)C)cc1 10.1021/jm300896d
44430723 86875 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 544 8 2 7 3.1 CNc1c(Nc2cc(Br)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232253 86875 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 544 8 2 7 3.1 CNc1c(Nc2cc(Br)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453200 95721 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2007.09.068
CHEMBL258065 95721 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2007.09.068
10555351 116222 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 586 4 1 3 7.3 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Br)ccc2Oc2ccc(Br)cc21 10.1021/jm0004244
CHEMBL33580 116222 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 586 4 1 3 7.3 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2cc(Br)ccc2Oc2ccc(Br)cc21 10.1021/jm0004244
73353555 91215 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 490 6 1 3 5.5 CO[C@]1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)C(C)C)CC1(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398752 91215 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 490 6 1 3 5.5 CO[C@]1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)C(C)C)CC1(C)C 10.1016/j.bmcl.2013.04.079
44309414 104106 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 10 3 5 3.1 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnnc2ccccc12 10.1016/j.bmcl.2004.02.021
CHEMBL309338 104106 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 10 3 5 3.1 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnnc2ccccc12 10.1016/j.bmcl.2004.02.021
57888812 82907 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 4 1 2 4.9 CC(C)(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180540 82907 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 4 1 2 4.9 CC(C)(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
24758045 82869 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 392 7 1 2 4.6 CC(C)CCC(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180502 82869 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 392 7 1 2 4.6 CC(C)CCC(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
44430713 86750 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL231829 86750 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44430756 87181 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2ccncc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232654 87181 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2ccncc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44309327 206399 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 446 9 3 5 3.0 NC(=O)[C@@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCC1 10.1016/j.bmcl.2004.02.021
CHEMBL69274 206399 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 446 9 3 5 3.0 NC(=O)[C@@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCC1 10.1016/j.bmcl.2004.02.021
17753030 87045 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232441 87045 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 486 7 2 7 2.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
10873705 99390 None 7 Human Binding pIC50 = 6.6 6.6 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.8 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL282285 99390 None 7 Human Binding pIC50 = 6.6 6.6 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.8 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00176-7
44309178 103148 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 466 10 3 5 3.3 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL307535 103148 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 466 10 3 5 3.3 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
57390926 67885 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 427 7 2 6 2.6 Cc1noc(C)c1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.013
CHEMBL1910159 67885 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 427 7 2 6 2.6 Cc1noc(C)c1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.013
57888925 82911 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 4 1 2 5.2 Cc1ccccc1C(=O)NC(C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)(C)C 10.1021/jm300896d
CHEMBL2180544 82911 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 4 1 2 5.2 Cc1ccccc1C(=O)NC(C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)(C)C 10.1021/jm300896d
57889874 82884 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 414 5 1 3 4.9 CC(C)C(NC(=O)Oc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180517 82884 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 414 5 1 3 4.9 CC(C)C(NC(=O)Oc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44309122 102875 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 482 11 4 6 3.4 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NO 10.1016/j.bmcl.2004.02.022
CHEMBL305423 102875 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 482 11 4 6 3.4 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NO 10.1016/j.bmcl.2004.02.022
25231300 174380 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 419 5 1 2 5.0 CCN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL454942 174380 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 419 5 1 2 5.0 CCN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
25231301 174470 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 405 4 1 2 4.6 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL455162 174470 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 405 4 1 2 4.6 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
44430716 86793 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 560 8 2 7 3.6 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Br)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232042 86793 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 560 8 2 7 3.6 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Br)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
10531632 11173 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 473 6 1 2 6.7 CCC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178571 11173 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 473 6 1 2 6.7 CCC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL33050 11173 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 473 6 1 2 6.7 CCC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
10507823 11179 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 475 6 1 2 6.8 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178590 11179 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 475 6 1 2 6.8 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL33614 11179 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 475 6 1 2 6.8 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
21071083 86920 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 4 0 5 3.2 COc1cccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c1 10.1016/j.bmcl.2013.01.005
CHEMBL2322872 86920 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 4 0 5 3.2 COc1cccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c1 10.1016/j.bmcl.2013.01.005
59278314 170021 None 24 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
CHEMBL4441094 170021 None 24 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 425 5 1 7 2.3 CS(=O)(=O)c1cc(CNC(=O)c2cncc3c2cnn3-c2ccc(F)cc2)ccn1 10.1016/j.bmcl.2018.12.024
24758044 82895 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180528 82895 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
10049340 102698 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 11 3 5 3.3 CC(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.021
10049340 102698 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 11 3 5 3.3 CC(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL304358 102698 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 11 3 5 3.3 CC(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.021
CHEMBL304358 102698 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 11 3 5 3.3 CC(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
44309105 206295 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 468 10 3 5 3.1 NC(=O)[C@H](Cc1ccccc1)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL68551 206295 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 468 10 3 5 3.1 NC(=O)[C@H](Cc1ccccc1)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
71460999 82913 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 5 3 4 2.3 CC(O)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180546 82913 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 5 3 4 2.3 CC(O)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
73355055 91217 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 427 5 1 3 4.5 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@H](c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398757 91217 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 427 5 1 3 4.5 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@H](c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
25233582 190211 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 401 5 1 3 4.0 COc1ccc(NC(=O)N2CCC[C@@H]2C(=O)N(C)Cc2ccc(Cl)cc2)cc1 10.1021/jm801416q
CHEMBL517290 190211 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 401 5 1 3 4.0 COc1ccc(NC(=O)N2CCC[C@@H]2C(=O)N(C)Cc2ccc(Cl)cc2)cc1 10.1021/jm801416q
44309213 206187 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 478 11 3 6 3.1 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(OC)cc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL67757 206187 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 478 11 3 6 3.1 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(OC)cc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
44430720 86872 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3cccc(F)c3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232251 86872 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3cccc(F)c3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
57888758 91195 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 486 6 3 4 3.9 CC(C)[C@@H](NC(=O)c1ccccc1C(=O)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398732 91195 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 486 6 3 4 3.9 CC(C)[C@@H](NC(=O)c1ccccc1C(=O)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
11828215 114523 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 613 12 3 3 7.1 O=C(NCCc1ccc(F)cc1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL333422 114523 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 613 12 3 3 7.1 O=C(NCCc1ccc(F)cc1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
25233753 177083 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1cccc(C(F)(F)F)c1 10.1021/jm801416q
CHEMBL462442 177083 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 439 4 1 2 5.0 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1cccc(C(F)(F)F)c1 10.1021/jm801416q
57889099 114532 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 449 5 3 3 4.1 CC(C)[C@@H](NC(=O)NC1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334725 114532 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 449 5 3 3 4.1 CC(C)[C@@H](NC(=O)NC1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57889314 91208 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 406 5 2 3 3.3 CC(C)[C@@H](NC(=O)C1CC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398745 91208 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 406 5 2 3 3.3 CC(C)[C@@H](NC(=O)C1CC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888900 91227 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 521 6 3 5 2.9 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398767 91227 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 521 6 3 5 2.9 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44537841 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889736 114534 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334727 114534 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57888785 114536 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334815 114536 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57889188 114537 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 437 6 3 3 3.9 CC[C@@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
CHEMBL3334816 114537 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 437 6 3 3 3.9 CC[C@@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
57991707 91185 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398722 91185 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10509339 12374 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 631 6 1 2 8.3 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1185511 12374 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 631 6 1 2 8.3 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL418589 12374 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 631 6 1 2 8.3 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
10094211 90810 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 430 6 3 6 2.1 CNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391794 90810 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 430 6 3 6 2.1 CNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.04.047
44537841 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
10393066 104382 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 447 6 4 6 2.7 NC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099948 104382 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 447 6 4 6 2.7 NC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
72945112 104395 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 445 6 4 6 2.5 CNC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099961 104395 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 445 6 4 6 2.5 CNC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
44537841 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57888895 91193 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398730 91193 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10676520 11176 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 617 5 1 2 7.9 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1178581 11176 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 617 5 1 2 7.9 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL33340 11176 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 617 5 1 2 7.9 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
57889023 91225 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 576 7 4 4 5.4 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398765 91225 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 576 7 4 4 5.4 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889764 91229 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 457 6 2 4 3.6 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398769 91229 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 457 6 2 4 3.6 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889843 91204 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 394 5 2 3 3.3 CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398741 91204 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 394 5 2 3 3.3 CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
10507823 11179 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 475 6 1 2 6.8 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178590 11179 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 475 6 1 2 6.8 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL33614 11179 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 475 6 1 2 6.8 CCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
73355055 91217 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 427 5 1 3 4.5 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@H](c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398757 91217 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 427 5 1 3 4.5 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@H](c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
21070989 86923 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
10652533 11175 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 603 4 1 2 7.5 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL1178579 11175 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 603 4 1 2 7.5 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
CHEMBL33223 11175 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 603 4 1 2 7.5 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Br)ccc3Oc3ccc(Br)cc32)CC1 10.1021/jm0004244
44431524 145370 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 476 8 2 5 2.7 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2C(=O)NCCN)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL391302 145370 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 476 8 2 5 2.7 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2C(=O)NCCN)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
24758044 82895 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2180528 82895 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
24758294 82863 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.4 CC(C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180496 82863 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.4 CC(C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453359 97613 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 408 7 2 4 3.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/j.bmcl.2007.09.068
CHEMBL270631 97613 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 408 7 2 4 3.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/j.bmcl.2007.09.068
21070989 86923 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in mouse WEHI274.1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in mouse WEHI274.1 cells
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in mouse WEHI274.1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in mouse WEHI274.1 cells
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44308902 103243 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
CHEMBL308243 103243 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 453 10 3 4 4.5 CNC(=O)[C@@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
57888688 82886 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 448 7 1 3 4.2 CC(C)C(NS(=O)(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180519 82886 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 448 7 1 3 4.2 CC(C)C(NS(=O)(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
1370410 86936 None 9 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 404 3 0 4 3.4 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322888 86936 None 9 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 404 3 0 4 3.4 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2013.01.005
512282 758 None 42 Human Binding pIC50 = 7.5 7.5 147 2
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.037
767 758 None 42 Human Binding pIC50 = 7.5 7.5 147 2
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.037
CHEMBL232656 758 None 42 Human Binding pIC50 = 7.5 7.5 147 2
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.037
10995218 16623 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 549 12 4 4 5.1 O=C(NCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL124127 16623 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 549 12 4 4 5.1 O=C(NCCCO)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
10974378 114361 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 664 12 3 4 7.4 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
CHEMBL333063 114361 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 664 12 3 4 7.4 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm0201767
10255511 90827 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 502 6 2 7 2.7 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCOCC1 10.1016/j.bmcl.2013.04.047
CHEMBL2391811 90827 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 502 6 2 7 2.7 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCOCC1 10.1016/j.bmcl.2013.04.047
25254218 16192 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1ncnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224120 16192 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 449 4 1 4 5.4 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCC[C@@H]1c1ncnn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
24758172 82876 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 2 4.8 Cc1ccccc1C(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180509 82876 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 2 4.8 Cc1ccccc1C(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
24758173 82892 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 378 6 1 2 4.2 CC(C)CC(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180525 82892 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 378 6 1 2 4.2 CC(C)CC(=O)N[C@@H](C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
11464915 104386 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 442 5 2 5 3.4 O=C1CCc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2N1 10.1016/j.bmcl.2013.11.062
CHEMBL3099952 104386 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 442 5 2 5 3.4 O=C1CCc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2N1 10.1016/j.bmcl.2013.11.062
68817337 87392 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 425 7 2 6 2.8 COc1ccc(NC(C)=O)c(OC[C@@H](N)CN2CCC3(CC2)Cc2ccccc2O3)c1 10.1016/j.bmcl.2012.12.095
CHEMBL2332939 87392 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 425 7 2 6 2.8 COc1ccc(NC(C)=O)c(OC[C@@H](N)CN2CCC3(CC2)Cc2ccccc2O3)c1 10.1016/j.bmcl.2012.12.095
44453161 95322 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.5 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL256271 95322 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.5 CC1CC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmcl.2007.09.068
21071096 86941 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 4 0 5 3.2 COc1ccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc1 10.1016/j.bmcl.2013.01.005
CHEMBL2322893 86941 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 416 4 0 5 3.2 COc1ccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc1 10.1016/j.bmcl.2013.01.005
57889972 82917 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 428 6 2 3 4.0 CC(C)CC(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180550 82917 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 428 6 2 3 4.0 CC(C)CC(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
21071106 86986 None 1 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 400 3 0 4 3.5 Cc1cccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c1 10.1016/j.bmcl.2013.01.005
CHEMBL2323422 86986 None 1 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 400 3 0 4 3.5 Cc1cccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c1 10.1016/j.bmcl.2013.01.005
71457362 82893 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 392 7 1 2 4.6 CC[C@@H](C)[C@@H](NC(=O)CC(C)C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180526 82893 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 392 7 1 2 4.6 CC[C@@H](C)[C@@H](NC(=O)CC(C)C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
21071046 86894 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 397 4 1 6 2.4 COc1cc(N2CCN(C(=O)Cn3nc(N)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322848 86894 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 397 4 1 6 2.4 COc1cc(N2CCN(C(=O)Cn3nc(N)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
21070990 86914 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 512 5 0 5 5.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3-c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322866 86914 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 512 5 0 5 5.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3-c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889407 91182 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](N)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398719 91182 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](N)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44309161 206500 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 9 3 6 2.3 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCOCC1 10.1016/j.bmcl.2004.02.022
CHEMBL69876 206500 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 9 3 6 2.3 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCOCC1 10.1016/j.bmcl.2004.02.022
24759081 82882 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 7 1 2 4.8 CC(C)C(NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180515 82882 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 7 1 2 4.8 CC(C)C(NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44430714 86751 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 482 8 2 7 2.8 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccccc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL231830 86751 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 482 8 2 7 2.8 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccccc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453503 95132 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccsc1 10.1016/j.bmcl.2007.09.068
CHEMBL255338 95132 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 490 8 2 5 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccsc1 10.1016/j.bmcl.2007.09.068
44453164 95787 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1OC(F)(F)F 10.1016/j.bmcl.2007.09.068
CHEMBL258361 95787 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1OC(F)(F)F 10.1016/j.bmcl.2007.09.068
10555108 11171 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 445 4 1 2 5.9 C[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178543 11171 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 445 4 1 2 5.9 C[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL32257 11171 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 445 4 1 2 5.9 C[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
44309166 206268 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 9 3 6 2.3 NC(=O)[C@@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCOCC1 10.1016/j.bmcl.2004.02.021
CHEMBL68368 206268 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 9 3 6 2.3 NC(=O)[C@@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCOCC1 10.1016/j.bmcl.2004.02.021
44453195 155266 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 496 4 1 4 4.8 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(C)(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL402327 155266 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 496 4 1 4 4.8 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(C)(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
24759191 82909 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 2 4.8 Cc1ccccc1C(=O)NC(C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180542 82909 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 2 4.8 Cc1ccccc1C(=O)NC(C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
44453400 95586 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 460 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL257509 95586 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 460 7 2 4 3.8 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1Cl 10.1016/j.bmcl.2007.09.068
11104005 117424 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 602 12 3 4 6.2 O=C(NCCN1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL339752 117424 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 602 12 3 4 6.2 O=C(NCCN1CCCCC1)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
11113940 79613 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 509 8 1 6 5.9 CCOc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 10.1016/s0960-894x(01)00176-7
CHEMBL21143 79613 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 509 8 1 6 5.9 CCOc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 10.1016/s0960-894x(01)00176-7
25231299 189157 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 433 6 1 2 5.4 CCCN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL509457 189157 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 433 6 1 2 5.4 CCCN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
44453226 95792 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 536 4 1 4 5.4 O=S(=O)(c1ccc(Cl)c(Cl)c1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL258369 95792 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 536 4 1 4 5.4 O=S(=O)(c1ccc(Cl)c(Cl)c1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
21071108 86940 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 400 3 0 4 3.5 Cc1ccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc1 10.1016/j.bmcl.2013.01.005
CHEMBL2322892 86940 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 400 3 0 4 3.5 Cc1ccc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc1 10.1016/j.bmcl.2013.01.005
57840518 86899 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)[C@H](C)C2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322852 86899 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)[C@H](C)C2)ccc1Cl 10.1016/j.bmcl.2013.01.005
69439557 104387 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 440 5 2 5 3.4 O=c1ccc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2[nH]1 10.1016/j.bmcl.2013.11.062
CHEMBL3099953 104387 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 440 5 2 5 3.4 O=c1ccc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2[nH]1 10.1016/j.bmcl.2013.11.062
57888963 82914 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 4 2 3 3.5 C/C=C(/NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180547 82914 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 4 2 3 3.5 C/C=C(/NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453290 97475 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL269956 97475 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10628025 11177 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 523 6 1 2 7.6 O=C(NC1CC[N+](Cc2ccccc2)(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL1178588 11177 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 523 6 1 2 7.6 O=C(NC1CC[N+](Cc2ccccc2)(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL33586 11177 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 523 6 1 2 7.6 O=C(NC1CC[N+](Cc2ccccc2)(CC2CCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
24740170 82903 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 433 5 1 3 4.1 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm300896d
CHEMBL2180536 82903 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 433 5 1 3 4.1 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm300896d
44431527 88021 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 448 7 1 4 3.6 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2CC(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL234262 88021 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 448 7 1 4 3.6 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2CC(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
71457361 82864 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 7 1 2 4.8 CC[C@@H](C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180497 82864 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 7 1 2 4.8 CC[C@@H](C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453265 95439 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2007.09.068
CHEMBL256821 95439 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2007.09.068
10579693 11172 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 489 7 1 2 7.2 CCCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178558 11172 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 489 7 1 2 7.2 CCCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL32713 11172 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 489 7 1 2 7.2 CCCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
57396208 67886 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 463 9 2 3 4.3 O=C(NCCCCN1CCC(Oc2ccc(F)cc2)C1)NCc1ccc(Br)cc1 10.1016/j.bmcl.2011.09.013
CHEMBL1910160 67886 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR1 expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 463 9 2 3 4.3 O=C(NCCCCN1CCC(Oc2ccc(F)cc2)C1)NCc1ccc(Br)cc1 10.1016/j.bmcl.2011.09.013
24759740 82904 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 364 5 1 2 3.8 CC(C)C(=O)NC(C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
CHEMBL2180537 82904 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 364 5 1 2 3.8 CC(C)C(=O)NC(C(=O)N1CCC(c2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm300896d
44453641 97989 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 438 8 2 5 3.0 COc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL272559 97989 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 438 8 2 5 3.0 COc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
3497 1181 None 25 Human Binding pIC50 = 7.4 7.4 2 3
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1016/j.bmcl.2018.11.015
5311123 1181 None 25 Human Binding pIC50 = 7.4 7.4 2 3
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1016/j.bmcl.2018.11.015
CHEMBL1628706 1181 None 25 Human Binding pIC50 = 7.4 7.4 2 3
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1016/j.bmcl.2018.11.015
44453157 155357 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL402827 155357 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
10164 874 None 26 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 451 4 1 8 2.2 COc1cc(ccc1Cl)N1CCN(CC1)C(=O)Cn1[nH]c(=C2N=CC=N2)c2c1nccc2 10.1016/j.bmcl.2018.11.015
135565361 874 None 26 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 451 4 1 8 2.2 COc1cc(ccc1Cl)N1CCN(CC1)C(=O)Cn1[nH]c(=C2N=CC=N2)c2c1nccc2 10.1016/j.bmcl.2018.11.015
CHEMBL4444976 874 None 26 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay
ChEMBL 451 4 1 8 2.2 COc1cc(ccc1Cl)N1CCN(CC1)C(=O)Cn1[nH]c(=C2N=CC=N2)c2c1nccc2 10.1016/j.bmcl.2018.11.015
118714001 114535 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334728 114535 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57889003 91189 None 5 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of HCC-1-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of HCC-1-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of HCC-1-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of HCC-1-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
21070989 86923 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889180 114533 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334726 114533 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57889897 91200 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 456 6 2 3 4.2 CC(C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398737 91200 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 456 6 2 3 4.2 CC(C)[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
24738063 91218 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 419 5 1 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CCN(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398758 91218 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 419 5 1 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CCN(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44537841 675 None 16 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [125I]hMIP-1alpha from CCR1 in human PBMCDisplacement of [125I]hMIP-1alpha from CCR1 in human PBMC
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [125I]hMIP-1alpha from CCR1 in human PBMCDisplacement of [125I]hMIP-1alpha from CCR1 in human PBMC
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [125I]hMIP-1alpha from CCR1 in human PBMCDisplacement of [125I]hMIP-1alpha from CCR1 in human PBMC
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [125I]hMIP-1alpha from CCR1 in human PBMCDisplacement of [125I]hMIP-1alpha from CCR1 in human PBMC
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [125I]hMIP-1alpha from CCR1 in human PBMCDisplacement of [125I]hMIP-1alpha from CCR1 in human PBMC
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889979 91198 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398735 91198 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889121 91205 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 408 5 2 3 3.6 CC(C)C(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398742 91205 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 408 5 2 3 3.6 CC(C)C(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
57889003 91189 None 5 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of ieukotactin-1-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of ieukotactin-1-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at human CCR1 assessed as inhibition of ieukotactin-1-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of ieukotactin-1-induced chemotaxis
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889843 91204 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 394 5 2 3 3.3 CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398741 91204 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 394 5 2 3 3.3 CCC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
72945310 104375 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 475 7 3 6 3.3 CNC(=O)Nc1ccc(OC)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099941 104375 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 475 7 3 6 3.3 CNC(=O)Nc1ccc(OC)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
57889121 91205 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 408 5 2 3 3.6 CC(C)C(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398742 91205 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 408 5 2 3 3.6 CC(C)C(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1016/j.bmcl.2013.04.079
57888747 91230 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccccc1Cl)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398770 91230 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccccc1Cl)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888938 91226 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 477 6 2 4 3.1 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398766 91226 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 477 6 2 4 3.1 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
57840427 86889 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 396 4 0 5 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322843 86889 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 396 4 0 5 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
24758171 82866 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 7 1 2 4.8 CC(C)[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180499 82866 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 7 1 2 4.8 CC(C)[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
24758856 82881 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.4 CC(C)C(NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180514 82881 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.4 CC(C)C(NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
10435088 90847 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 475 8 4 7 1.9 NCCNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391936 90847 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 475 8 4 7 1.9 NCCNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
44453579 155678 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.5 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404465 155678 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.5 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
25233577 176879 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 419 4 1 2 5.0 Cc1cc(CN(C)C(=O)[C@H]2CCCN2C(=O)Nc2ccc(Cl)cc2)ccc1Cl 10.1021/jm801416q
CHEMBL460535 176879 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 419 4 1 2 5.0 Cc1cc(CN(C)C(=O)[C@H]2CCCN2C(=O)Nc2ccc(Cl)cc2)ccc1Cl 10.1021/jm801416q
59444242 170237 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 414 5 2 3 3.6 CC1(C)CN(C(=O)CCNC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL4444092 170237 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 414 5 2 3 3.6 CC1(C)CN(C(=O)CCNC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
44453437 160934 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL411477 160934 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.068
44537841 675 None 16 Human Binding pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hrAntagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
59444197 170197 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 420 5 2 3 3.7 CC(CNC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL4443458 170197 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 420 5 2 3 3.7 CC(CNC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
44430755 153514 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL397910 153514 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 577 10 2 8 3.9 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2cccnc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
71717437 86930 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 494 5 1 6 3.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C(=O)O)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322882 86930 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 494 5 1 6 3.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C(=O)O)c1Cl 10.1016/j.bmcl.2013.01.005
44453321 97543 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1c(Cl)cccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL270254 97543 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1c(Cl)cccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44309171 206492 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 12 3 5 3.7 CC(C)CCC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.021
CHEMBL69816 206492 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 462 12 3 5 3.7 CC(C)CCC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.021
9979012 79833 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 411 7 1 5 4.4 O=C(CSc1nc2ccccc2s1)NCC1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(01)00176-7
CHEMBL21199 79833 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 411 7 1 5 4.4 O=C(CSc1nc2ccccc2s1)NCC1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(01)00176-7
44453198 95670 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 516 4 1 4 5.2 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL257853 95670 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 516 4 1 4 5.2 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2c(Cl)cccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
44309222 164160 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 414 10 3 5 2.9 CC[C@H](C)[C@H](NC(=O)c1cnc2ccccc2n1)[C@@H](O)C[C@@H](CC(C)C)C(=O)NC 10.1016/j.bmcl.2004.02.021
CHEMBL420924 164160 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 414 10 3 5 2.9 CC[C@H](C)[C@H](NC(=O)c1cnc2ccccc2n1)[C@@H](O)C[C@@H](CC(C)C)C(=O)NC 10.1016/j.bmcl.2004.02.021
57889002 82900 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 382 5 1 2 4.0 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm300896d
CHEMBL2180533 82900 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 382 5 1 2 4.0 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm300896d
59444291 174252 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 477 6 3 4 3.0 CC(=O)N[C@@H]1CC[C@@H](C(=O)N[C@H](C)CC(=O)N2CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C2)C1 nan
CHEMBL4546558 174252 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 477 6 3 4 3.0 CC(=O)N[C@@H]1CC[C@@H](C(=O)N[C@H](C)CC(=O)N2CC[C@](O)(c3ccc(Cl)cc3)C(C)(C)C2)C1 nan
44453199 95720 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 422 7 2 4 3.3 Cc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL258064 95720 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 422 7 2 4 3.3 Cc1ccc(S(=O)(=O)NCCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.09.068
44453466 155739 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404757 155739 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453639 158956 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL409498 158956 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.4 Cc1cccc(Cl)c1S(=O)(=O)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
25231302 177110 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 435 6 2 3 4.0 O=C([C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1)N(CCO)Cc1ccccc1Cl 10.1021/jm801416q
CHEMBL462650 177110 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 435 6 2 3 4.0 O=C([C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1)N(CCO)Cc1ccccc1Cl 10.1021/jm801416q
44431528 145277 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 541 9 1 7 2.5 COS(=O)(=O)NC(=O)Cc1cc(Cl)ccc1OCC(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2007.03.037
CHEMBL391239 145277 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 541 9 1 7 2.5 COS(=O)(=O)NC(=O)Cc1cc(Cl)ccc1OCC(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C 10.1016/j.bmcl.2007.03.037
24758517 82825 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 430 6 1 2 4.6 CC(C)[C@@H](NC(=O)Cc1cccc(F)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180187 82825 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 430 6 1 2 4.6 CC(C)[C@@H](NC(=O)Cc1cccc(F)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453501 97859 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL271903 97859 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Br)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44309244 102119 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 516 9 3 5 4.7 CC1(C)CC([C@H](C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)C(N)=O)CC(C)(C)C1 10.1016/j.bmcl.2004.02.021
CHEMBL302038 102119 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 516 9 3 5 4.7 CC1(C)CC([C@H](C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)C(N)=O)CC(C)(C)C1 10.1016/j.bmcl.2004.02.021
24758518 82520 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 446 6 1 2 5.1 CC(C)[C@@H](NC(=O)Cc1cccc(Cl)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2177135 82520 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 446 6 1 2 5.1 CC(C)[C@@H](NC(=O)Cc1cccc(Cl)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57889478 82860 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.9 CC[C@@H](C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180493 82860 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 6 1 2 4.9 CC[C@@H](C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
70861827 176275 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 433 5 2 4 3.6 CC(C)(CC(=O)N1CCC(O)(c2ccc(C#N)cc2)C(C)(C)C1)NC(=O)c1ccccc1 nan
CHEMBL4593102 176275 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 433 5 2 4 3.6 CC(C)(CC(=O)N1CCC(O)(c2ccc(C#N)cc2)C(C)(C)C1)NC(=O)c1ccccc1 nan
11037958 75998 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm300682j
CHEMBL20532 75998 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm300682j
11037958 75998 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL20532 75998 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 465 6 1 5 5.5 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(01)00176-7
57889003 91189 None 5 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of MIP1alpha-induced upregulation of beta2-integrin CD11bAntagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of MIP1alpha-induced upregulation of beta2-integrin CD11b
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of MIP1alpha-induced upregulation of beta2-integrin CD11bAntagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of MIP1alpha-induced upregulation of beta2-integrin CD11b
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888690 82870 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 376 6 1 2 4.0 CC(C)[C@@H](NC(=O)CC1CC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180503 82870 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 376 6 1 2 4.0 CC(C)[C@@H](NC(=O)CC1CC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44309353 103459 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL308473 103459 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
59444274 176246 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 535 6 3 5 4.4 C[C@H](CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)[C@@H]1CC[C@@H](NC(=O)OC(C)(C)C)C1 nan
CHEMBL4592423 176246 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 535 6 3 5 4.4 C[C@H](CC(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)NC(=O)[C@@H]1CC[C@@H](NC(=O)OC(C)(C)C)C1 nan
44453615 95217 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
CHEMBL255797 95217 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC[C@H](N2CCC(O)(c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2007.09.068
44309128 206484 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 422 10 4 6 1.2 NC(=O)[C@H](CCO)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL69735 206484 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 422 10 4 6 1.2 NC(=O)[C@H](CCO)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
57840515 86917 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 493 6 0 6 3.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CN(C)C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322869 86917 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 493 6 0 6 3.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CN(C)C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
6918497 113493 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
25233578 190185 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 419 4 1 2 5.2 CC(c1ccc(Cl)cc1)N(C)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL517262 190185 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 419 4 1 2 5.2 CC(c1ccc(Cl)cc1)N(C)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1 10.1021/jm801416q
57889613 91222 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 432 5 2 3 4.3 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398762 91222 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 432 5 2 3 4.3 CC(C)[C@@H](NC(=O)c1ccc(F)c(O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
57889023 91225 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 576 7 4 4 5.4 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398765 91225 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 576 7 4 4 5.4 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44309318 103046 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 460 10 3 5 3.4 NC(=O)[C@H](CC1CCCC1)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL306685 103046 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 460 10 3 5 3.4 NC(=O)[C@H](CC1CCCC1)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
9889700 118652 None 11 Human Binding pIC50 = 7.3 7.3 - 1
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0004244
CHEMBL34166 118652 None 11 Human Binding pIC50 = 7.3 7.3 - 1
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0004244
44431523 88096 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 468 11 4 6 3.0 CC(C)(O)CC[C@@H](CN)C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2007.03.037
CHEMBL234606 88096 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 468 11 4 6 3.0 CC(C)(O)CC[C@@H](CN)C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2007.03.037
602123 83818 None 43 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
CHEMBL2205803 83818 None 43 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
68962095 90815 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 500 6 2 6 3.1 Cc1ccc(C(=O)N2CC[C@H](O)C2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2013.04.047
CHEMBL2391799 90815 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 500 6 2 6 3.1 Cc1ccc(C(=O)N2CC[C@H](O)C2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2013.04.047
57840437 86905 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 434 4 0 5 3.4 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(F)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322858 86905 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 434 4 0 5 3.4 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(F)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
71717436 86927 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 468 4 0 5 4.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(F)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322879 86927 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 468 4 0 5 4.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(F)c1Cl 10.1016/j.bmcl.2013.01.005
10579693 11172 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 489 7 1 2 7.2 CCCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178558 11172 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 489 7 1 2 7.2 CCCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL32713 11172 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 489 7 1 2 7.2 CCCC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
44537841 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2013.04.079
57889181 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2013.04.079
9497 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2013.04.079
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1016/j.bmcl.2013.04.079
9894714 11991 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 461 5 1 2 6.4 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1183117 11991 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 461 5 1 2 6.4 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL280751 11991 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 461 5 1 2 6.4 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
52916803 171085 None 20 Human Binding pIC50 = 8.3 8.3 - 1
Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000352a CCR1Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000352a CCR1
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL5210307
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 8.3 8.3 - 1
Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000352a CCR1Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000352a CCR1
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL5210307
52916803 171085 None 20 Human Binding pIC50 = 8.3 8.3 - 1
Scintillation Proximity Assay bindingScintillation Proximity Assay binding
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 8.3 8.3 - 1
Scintillation Proximity Assay bindingScintillation Proximity Assay binding
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
44537841 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57888895 91193 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398730 91193 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccc(Cl)cc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
512282 758 None 42 Human Binding pIC50 = 8.3 8.3 147 2
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm801416q
767 758 None 42 Human Binding pIC50 = 8.3 8.3 147 2
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm801416q
CHEMBL232656 758 None 42 Human Binding pIC50 = 8.3 8.3 147 2
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm801416q
71681399 91187 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1N)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398724 91187 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 449 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CCC[C@@H]1N)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10482996 104384 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 449 6 3 5 3.2 NC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099950 104384 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 449 6 3 5 3.2 NC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
57889758 91201 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 470 7 2 3 4.6 CC(C)[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398738 91201 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 470 7 2 3 4.6 CC(C)[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
6918497 113493 None 1 Mouse Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against 125 I -MIP-1 alpha binding to mouse CCR1 receptorsInhibitory activity against 125 I -MIP-1 alpha binding to mouse CCR1 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against 125 I -MIP-1 alpha binding to mouse CCR1 receptorsInhibitory activity against 125 I -MIP-1 alpha binding to mouse CCR1 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against 125 I -MIP-1 alpha binding to mouse CCR1 receptorsInhibitory activity against 125 I -MIP-1 alpha binding to mouse CCR1 receptors
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
6918497 113493 None 1 Mouse Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
11236656 86916 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 1 6 3.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CN)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322868 86916 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 465 5 1 6 3.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CN)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
24782574 179468 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 453 4 1 2 5.3 Cc1cc(C(F)(F)F)ccc1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL473734 179468 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 453 4 1 2 5.3 Cc1cc(C(F)(F)F)ccc1NC(=O)N1CCC[C@@H]1C(=O)N(C)Cc1ccc(Cl)cc1 10.1021/jm801416q
24758744 82862 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 6 1 2 4.2 CC[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180495 82862 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 6 1 2 4.2 CC[C@@H](NC(=O)Cc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44430753 142110 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387608 142110 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 598 11 3 9 2.2 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCNCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
57840557 86910 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 473 5 1 6 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(NC(C)=O)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322862 86910 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 473 5 1 6 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(NC(C)=O)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44453292 155569 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 448 4 1 4 3.8 Cc1ccccc1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404033 155569 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 448 4 1 4 3.8 Cc1ccccc1S(=O)(=O)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
11072275 16804 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 632 10 3 5 5.9 COC(=O)N1CCC(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0201767
CHEMBL124585 16804 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 632 10 3 5 5.9 COC(=O)N1CCC(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm0201767
9889700 118652 None 11 Mouse Binding pIC50 = 5.3 5.3 - 1
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0004244
CHEMBL34166 118652 None 11 Mouse Binding pIC50 = 5.3 5.3 - 1
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0004244
602123 83818 None 43 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
CHEMBL2205803 83818 None 43 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 236 2 0 4 2.4 O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 10.1021/jm301121j
77865 107342 None 51 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL317115 107342 None 51 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
10670301 114175 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 430 4 1 3 5.8 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL33277 114175 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 430 4 1 3 5.8 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
44453469 95786 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL258360 95786 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2007.09.068
44453499 155493 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403613 155493 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 486 4 1 4 4.3 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(F)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44309236 206105 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 475 10 3 4 3.3 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cncc(Br)c1 10.1016/j.bmcl.2004.02.021
CHEMBL67256 206105 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 475 10 3 4 3.3 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cncc(Br)c1 10.1016/j.bmcl.2004.02.021
11794863 118954 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 392 7 1 3 5.1 CCCCCCN1CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
CHEMBL34226 118954 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 392 7 1 3 5.1 CCCCCCN1CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1016/j.ejmech.2020.113085
11794863 118954 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 392 7 1 3 5.1 CCCCCCN1CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL34226 118954 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 392 7 1 3 5.1 CCCCCCN1CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
77865 107342 None 51 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
CHEMBL317115 107342 None 51 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 214 0 0 2 3.4 Clc1cc2cccnc2c2ncccc12 10.1021/jm301121j
10793529 109810 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 588 4 1 3 7.4 O=C(NC1CCN(CC2CCCCCCC2)CC1)C1c2cc(Br)ccc2Oc2ccc(Br)cc21 10.1021/jm0004244
CHEMBL32305 109810 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 588 4 1 3 7.4 O=C(NC1CCN(CC2CCCCCCC2)CC1)C1c2cc(Br)ccc2Oc2ccc(Br)cc21 10.1021/jm0004244
44453197 155503 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.5 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403665 155503 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 482 4 1 4 4.5 CC1(N2CCC(O)(c3ccc(Cl)cc3)CC2)CCN(S(=O)(=O)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
44309112 206401 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cncc2ccccc12 10.1016/j.bmcl.2004.02.021
CHEMBL69285 206401 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cncc2ccccc12 10.1016/j.bmcl.2004.02.021
71719856 86931 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 493 5 1 6 3.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C(N)=O)c1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322883 86931 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 493 5 1 6 3.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)cc(C(N)=O)c1Cl 10.1016/j.bmcl.2013.01.005
44309313 102582 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1ccccc1F)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL304053 102582 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 482 11 4 6 2.5 CC(C)(O)CCC(C[C@H](O)[C@H](Cc1ccccc1F)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
57840210 86898 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 5 1 6 2.6 COc1cc(N2CCN(C(=O)Cn3nc(C(=O)O)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322851 86898 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 5 1 6 2.6 COc1cc(N2CCN(C(=O)Cn3nc(C(=O)O)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
57889880 82916 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 414 6 2 3 3.7 CCCC(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180549 82916 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 414 6 2 3 3.7 CCCC(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
24740167 82902 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 399 5 1 3 3.4 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180535 82902 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 399 5 1 3 3.4 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57889006 82918 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 446 7 2 4 3.7 CSCCC(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180551 82918 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 446 7 2 4 3.7 CSCCC(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57889003 91189 None 5 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of LKN1-induced upregulation of beta2-integrin CD11bAntagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of LKN1-induced upregulation of beta2-integrin CD11b
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398726 91189 None 5 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of LKN1-induced upregulation of beta2-integrin CD11bAntagonist activity at CCR1 in whole blood (unknown origin) assessed as inhibition of LKN1-induced upregulation of beta2-integrin CD11b
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
25233947 174377 None 5 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 435 6 2 3 4.0 O=C([C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1)N(CCO)Cc1ccc(Cl)cc1 10.1021/jm801416q
CHEMBL454940 174377 None 5 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 435 6 2 3 4.0 O=C([C@H]1CCCN1C(=O)Nc1ccc(Cl)cc1)N(CCO)Cc1ccc(Cl)cc1 10.1021/jm801416q
44453435 97654 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL270863 97654 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2007.09.068
44309407 103019 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 476 9 4 6 2.5 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCCCC1 10.1016/j.bmcl.2004.02.022
CHEMBL306457 103019 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 476 9 4 6 2.5 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCCCC1 10.1016/j.bmcl.2004.02.022
57889346 82889 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 441 7 2 2 4.6 CC(C)[C@@H](NC(=O)NCCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180522 82889 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 441 7 2 2 4.6 CC(C)[C@@H](NC(=O)NCCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
57888953 82901 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 1 2 4.5 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180534 82901 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 1 2 4.5 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
24758044 82895 None 0 Rabbit Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in rabbit PBMCs incubated for 60 minsDisplacement of [125I]MIP-1alpha from CCR1 in rabbit PBMCs incubated for 60 mins
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180528 82895 None 0 Rabbit Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from CCR1 in rabbit PBMCs incubated for 60 minsDisplacement of [125I]MIP-1alpha from CCR1 in rabbit PBMCs incubated for 60 mins
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44309061 163699 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 449 11 3 6 1.8 CN(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.021
CHEMBL420359 163699 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 449 11 3 6 1.8 CN(C)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.021
69437285 104388 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 457 5 3 6 2.1 O=c1[nH]c(=O)c2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2[nH]1 10.1016/j.bmcl.2013.11.062
CHEMBL3099954 104388 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 457 5 3 6 2.1 O=c1[nH]c(=O)c2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2[nH]1 10.1016/j.bmcl.2013.11.062
68816399 104393 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 423 5 2 5 2.8 N[C@H](COc1cccc2ccc(=O)[nH]c12)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099959 104393 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 423 5 2 5 2.8 N[C@H](COc1cccc2ccc(=O)[nH]c12)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
44309219 102167 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 512 9 4 6 2.8 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
CHEMBL302320 102167 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 512 9 4 6 2.8 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1(O)CCC(F)(F)CC1 10.1016/j.bmcl.2004.02.022
21071066 86937 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 386 3 0 4 3.2 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322889 86937 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 386 3 0 4 3.2 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2013.01.005
44309077 206786 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 549 11 2 6 3.6 CN1CCN(C(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2004.02.022
CHEMBL71499 206786 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 549 11 2 6 3.6 CN1CCN(C(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2004.02.022
21071098 86984 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 431 4 0 6 3.1 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2323420 86984 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 431 4 0 6 3.1 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmcl.2013.01.005
44453528 97593 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1016/j.bmcl.2007.09.068
CHEMBL270564 97593 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 414 7 2 5 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1016/j.bmcl.2007.09.068
25231481 177109 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 385 4 1 2 4.3 Cc1ccc(CN(C)C(=O)[C@H]2CCCN2C(=O)Nc2ccc(Cl)cc2)cc1 10.1021/jm801416q
CHEMBL462644 177109 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 385 4 1 2 4.3 Cc1ccc(CN(C)C(=O)[C@H]2CCCN2C(=O)Nc2ccc(Cl)cc2)cc1 10.1021/jm801416q
24758175 82834 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 454 5 1 3 5.7 CC(C)[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180196 82834 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 454 5 1 3 5.7 CC(C)[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453228 95451 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1F 10.1016/j.bmcl.2007.09.068
CHEMBL256888 95451 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1F 10.1016/j.bmcl.2007.09.068
44309235 102168 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1nccc2ccccc12 10.1016/j.bmcl.2004.02.021
CHEMBL302328 102168 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1nccc2ccccc12 10.1016/j.bmcl.2004.02.021
44309194 205997 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 464 11 4 6 2.4 CC(C)(O)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL66457 205997 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 464 11 4 6 2.4 CC(C)(O)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
25174628 130338 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679649 130338 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174628 130338 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679649 130338 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
44453084 95321 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 422 6 2 3 4.6 O=C(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
CHEMBL256264 95321 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 422 6 2 3 4.6 O=C(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.09.068
11166434 145369 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 434 6 1 4 3.7 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2C(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL391301 145369 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 434 6 1 4 3.7 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2C(=O)O)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
10670301 114175 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 430 4 1 3 5.8 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL33277 114175 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 430 4 1 3 5.8 O=C(NC1CCN(C/C2=C/CCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
44537841 675 None 16 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57888785 114536 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334815 114536 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 465 5 4 4 3.0 CC(C)[C@@H](NC(=O)N[C@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57889188 114537 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 437 6 3 3 3.9 CC[C@@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
CHEMBL3334816 114537 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 437 6 3 3 3.9 CC[C@@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C 10.1021/jm5003167
118714037 114544 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334823 114544 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57840302 86909 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 441 4 0 6 3.1 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(C#N)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322861 86909 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 441 4 0 6 3.1 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(C#N)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
21070989 86923 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human monocytesDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human monocytes
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human monocytesDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human monocytes
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
11397004 87390 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 459 7 2 6 3.5 COc1ccc(NC(C)=O)c(OC[C@@H](N)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2012.12.095
CHEMBL2332937 87390 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 459 7 2 6 3.5 COc1ccc(NC(C)=O)c(OC[C@@H](N)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 10.1016/j.bmcl.2012.12.095
57889979 91198 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398735 91198 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57889974 91190 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398727 91190 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 450 5 3 4 3.1 CC(C)[C@@H](NC(=O)[C@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888747 91230 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccccc1Cl)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398770 91230 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1ccccc1Cl)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10030344 104383 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 431 6 3 5 3.0 NC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099949 104383 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 431 6 3 5 3.0 NC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.11.062
57889484 91224 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 532 7 3 3 5.7 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398764 91224 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 532 7 3 3 5.7 CC(C)[C@@H](NC(=O)c1cccc(-c2ccccc2NC(N)=O)c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
44453584 97976 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 484 8 2 4 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.068
CHEMBL272523 97976 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 484 8 2 4 4.7 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.068
44453557 155642 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 451 7 1 4 4.2 N#CC1(c2ccc(Cl)cc2)CCN(CCCNS(=O)(=O)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL404301 155642 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 451 7 1 4 4.2 N#CC1(c2ccc(Cl)cc2)CCN(CCCNS(=O)(=O)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.09.068
44309192 103238 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 464 10 4 6 2.8 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(O)cc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL308209 103238 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 464 10 4 6 2.8 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccc(O)cc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
512282 758 None 42 Mouse Binding pIC50 = 6.2 6.2 -147 2
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
767 758 None 42 Mouse Binding pIC50 = 6.2 6.2 -147 2
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
CHEMBL232656 758 None 42 Mouse Binding pIC50 = 6.2 6.2 -147 2
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1016/j.bmcl.2007.03.104
44430713 86750 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL231829 86750 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 500 8 2 7 3.0 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
57888949 82887 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 413 5 2 2 4.9 CC(C)[C@@H](NC(=O)Nc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180520 82887 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 413 5 2 2 4.9 CC(C)[C@@H](NC(=O)Nc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44430745 142138 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 544 11 2 8 3.0 COCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL387822 142138 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 544 11 2 8 3.0 COCCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
10698568 11184 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178613 11184 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL34732 11184 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 459 5 1 2 6.3 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
9889700 118652 None 11 Human Binding pIC50 = 6.2 6.2 - 1
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL34166 118652 None 11 Human Binding pIC50 = 6.2 6.2 - 1
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44537841 675 None 16 Dog Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]hMIP-1alpha from dog PBMC CCR1Displacement of [125I]hMIP-1alpha from dog PBMC CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Dog Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]hMIP-1alpha from dog PBMC CCR1Displacement of [125I]hMIP-1alpha from dog PBMC CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Dog Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]hMIP-1alpha from dog PBMC CCR1Displacement of [125I]hMIP-1alpha from dog PBMC CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Dog Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]hMIP-1alpha from dog PBMC CCR1Displacement of [125I]hMIP-1alpha from dog PBMC CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Dog Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]hMIP-1alpha from dog PBMC CCR1Displacement of [125I]hMIP-1alpha from dog PBMC CCR1
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
44430750 87290 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 583 11 2 8 3.4 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL233042 87290 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 583 11 2 8 3.4 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN2CCCC2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44309074 206302 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 10 3 5 3.1 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL68581 206302 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 448 10 3 5 3.1 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
58778007 86985 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 6 2.6 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2323421 86985 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 6 2.6 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2013.01.005
49865900 16190 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 448 4 1 3 6.0 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCCC1c1nccn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224118 16190 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 448 4 1 3 6.0 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCCC1c1nccn1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
10049290 206426 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
10049290 206426 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.021
CHEMBL69411 206426 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.020
CHEMBL69411 206426 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 447 10 3 4 3.7 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2c1 10.1016/j.bmcl.2004.02.021
71453837 82867 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 8 1 2 5.2 CC[C@@H](C)[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180500 82867 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 8 1 2 5.2 CC[C@@H](C)[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
9894714 11991 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 461 5 1 2 6.4 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1183117 11991 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 461 5 1 2 6.4 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL280751 11991 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 461 5 1 2 6.4 CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
11813735 118209 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 562 12 3 4 5.3 CN(C)CCNC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL340797 118209 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 562 12 3 4 5.3 CN(C)CCNC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
44309185 206849 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 454 10 3 5 3.9 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
CHEMBL71903 206849 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 454 10 3 5 3.9 CNC(=O)[C@H](CC(C)C)C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.021
10555551 11174 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 473 6 1 2 6.6 C=CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178575 11174 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 473 6 1 2 6.6 C=CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL33104 11174 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 473 6 1 2 6.6 C=CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
71570634 87395 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 411 6 3 6 2.5 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1ccccc1O2 10.1016/j.bmcl.2012.12.095
CHEMBL2332942 87395 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 411 6 3 6 2.5 CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1ccccc1O2 10.1016/j.bmcl.2012.12.095
57840380 86918 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 507 6 1 6 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CNC(C)=O)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322870 86918 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 507 6 1 6 3.2 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3CNC(C)=O)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
25233579 176986 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 385 4 1 2 4.3 Cc1ccc(NC(=O)N2CCC[C@@H]2C(=O)N(C)Cc2ccc(Cl)cc2)cc1 10.1021/jm801416q
CHEMBL461590 176986 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 385 4 1 2 4.3 Cc1ccc(NC(=O)N2CCC[C@@H]2C(=O)N(C)Cc2ccc(Cl)cc2)cc1 10.1021/jm801416q
44453363 97579 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2007.09.068
CHEMBL270433 97579 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 458 7 2 4 4.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2007.09.068
49865951 16206 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 463 4 1 4 5.7 Cc1nnc([C@H]2CCCN2C(=O)Nc2ccc(C(F)(F)F)cc2)n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
CHEMBL1224189 16206 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 463 4 1 4 5.7 Cc1nnc([C@H]2CCCN2C(=O)Nc2ccc(C(F)(F)F)cc2)n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2010.07.082
118714035 114542 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334821 114542 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins
ChEMBL 439 6 4 4 2.5 CC(C)[C@@H](NC(=O)NC[C@H](C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
57840482 86908 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 542 4 0 5 3.8 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(I)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322860 86908 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 542 4 0 5 3.8 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(I)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44430758 142897 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 482 6 2 6 3.1 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL389293 142897 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 482 6 2 6 3.1 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)/C=C/c1ccc(Cl)cc1Nc1c(N)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44309286 102389 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 512 9 4 6 3.7 O=C(N[C@@H](Cc1ccccc1)[C@@H](O)CC(C(=O)NO)C1CCC(F)(F)CC1)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
CHEMBL303673 102389 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 512 9 4 6 3.7 O=C(N[C@@H](Cc1ccccc1)[C@@H](O)CC(C(=O)NO)C1CCC(F)(F)CC1)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
44309143 205949 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 481 11 4 6 2.9 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NN 10.1016/j.bmcl.2004.02.022
CHEMBL66159 205949 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 481 11 4 6 2.9 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NN 10.1016/j.bmcl.2004.02.022
68956901 90825 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 500 6 2 6 3.9 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCCCC1 10.1016/j.bmcl.2013.04.047
CHEMBL2391809 90825 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 500 6 2 6 3.9 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CCCCC1 10.1016/j.bmcl.2013.04.047
57889649 91196 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 486 6 3 4 3.9 CC(C)[C@@H](NC(=O)c1cccc(C(=O)O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398733 91196 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 486 6 3 4 3.9 CC(C)[C@@H](NC(=O)c1cccc(C(=O)O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
69435853 104385 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 444 5 2 6 2.9 O=C1COc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2N1 10.1016/j.bmcl.2013.11.062
CHEMBL3099951 104385 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 444 5 2 6 2.9 O=C1COc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2N1 10.1016/j.bmcl.2013.11.062
73350585 91181 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 441 5 2 4 3.4 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C2(CC2)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398718 91181 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 441 5 2 4 3.4 CC(C)[C@@H](NC(=O)c1cccnc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C2(CC2)C1 10.1016/j.bmcl.2013.04.079
44537841 675 None 16 Human Binding pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889291 91199 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1ccncc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398736 91199 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 443 5 2 4 3.6 CC(C)[C@@H](NC(=O)c1ccncc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10368788 90812 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 502 6 3 7 2.5 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@@H](O)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391796 90812 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 502 6 3 7 2.5 O=C(c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@@H](O)C1 10.1016/j.bmcl.2013.04.047
11764610 90822 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 516 7 2 7 3.1 CO[C@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391806 90822 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 516 7 2 7 3.1 CO[C@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
57889883 82831 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 444 7 1 2 5.0 CC(C)[C@@H](NC(=O)CCc1ccc(F)cc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180193 82831 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 444 7 1 2 5.0 CC(C)[C@@H](NC(=O)CCc1ccc(F)cc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
24758047 82868 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 390 5 1 2 4.4 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180501 82868 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 390 5 1 2 4.4 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
25233580 189939 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 389 4 1 2 4.1 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(F)cc1 10.1021/jm801416q
CHEMBL516495 189939 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 389 4 1 2 4.1 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(F)cc1 10.1021/jm801416q
44453502 155233 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL402110 155233 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 468 4 1 4 4.1 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10391877 90846 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 517 9 4 7 2.1 CC(=O)NCCNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
CHEMBL2391935 90846 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 517 9 4 7 2.1 CC(=O)NCCNC(=O)c1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 10.1016/j.bmcl.2013.04.047
11734303 168680 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 547 9 3 3 6.5 CC(C)(C)NC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL435812 168680 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 547 9 3 3 6.5 CC(C)(C)NC(=O)NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
10580015 11181 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 515 4 1 2 7.3 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL1178597 11181 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 515 4 1 2 7.3 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL33929 11181 None 0 Mouse Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 515 4 1 2 7.3 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
10000888 76004 None 1 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 397 6 1 5 4.2 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(01)00176-7
CHEMBL20539 76004 None 1 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
ChEMBL 397 6 1 5 4.2 O=C(CSc1nc2ccccc2s1)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(01)00176-7
44430732 87982 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 514 9 2 7 3.4 CCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL234073 87982 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 514 9 2 7 3.4 CCNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
25233581 177082 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 396 4 1 3 3.9 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C#N)cc1 10.1021/jm801416q
CHEMBL462441 177082 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cellsDisplacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
ChEMBL 396 4 1 3 3.9 CN(Cc1ccc(Cl)cc1)C(=O)[C@H]1CCCN1C(=O)Nc1ccc(C#N)cc1 10.1021/jm801416q
57840522 86912 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 504 4 0 5 4.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C(F)(F)F)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322864 86912 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 504 4 0 5 4.6 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C(F)(F)F)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
6918497 113493 None 1 Mouse Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL277930 113493 None 1 Mouse Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
CHEMBL331897 113493 None 1 Mouse Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.
ChEMBL 527 5 1 2 7.6 CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm0004244
12425 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
1318 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
CHEMBL415879 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
DB02365 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
44309364 206378 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 494 12 3 5 4.0 CCNC(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
CHEMBL69123 206378 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 494 12 3 5 4.0 CCNC(=O)C(CCC(C)(C)F)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2004.02.022
44430759 87182 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 496 7 2 6 3.6 CNc1c(Nc2cc(Cl)ccc2/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232655 87182 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 496 7 2 6 3.6 CNc1c(Nc2cc(Cl)ccc2/C=C/C(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
10623381 16909 None 0 Human Binding pIC50 = 6.1 6.1 - 1
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 448 8 2 3 5.3 NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
CHEMBL125111 16909 None 0 Human Binding pIC50 = 6.1 6.1 - 1
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 448 8 2 3 5.3 NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm0201767
25174463 130336 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 422 4 3 4 2.5 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CO)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679647 130336 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 422 4 3 4 2.5 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CO)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174463 130336 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 422 4 3 4 2.5 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CO)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679647 130336 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 422 4 3 4 2.5 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CO)CC[C@]1(O)c1ccc(Cl)cc1 nan
21070984 86925 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 478 5 0 5 4.7 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(Cl)c(OC(C)C)c2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322877 86925 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 478 5 0 5 4.7 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(Cl)c(OC(C)C)c2)CC1 10.1016/j.bmcl.2013.01.005
24758044 82895 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2180528 82895 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 398 5 1 2 4.5 CC(C)[C@@H](NC(=O)c1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
44430715 144604 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 516 8 2 7 3.5 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Cl)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL390706 144604 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 516 8 2 7 3.5 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(Cl)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453402 95626 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2007.09.068
CHEMBL257698 95626 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2007.09.068
11072063 16612 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 597 11 3 4 7.2 COc1ccc(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm0201767
CHEMBL124084 16612 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 597 11 3 4 7.2 COc1ccc(NC(=O)NCC(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm0201767
59444266 174808 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 477 5 2 4 4.4 CC(C)(CC(=O)N1CCC(O)(c2ncc(Cl)cc2Cl)C(C)(C)C1)NC(=O)c1ccccc1 nan
CHEMBL4559773 174808 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 477 5 2 4 4.4 CC(C)(CC(=O)N1CCC(O)(c2ncc(Cl)cc2Cl)C(C)(C)C1)NC(=O)c1ccccc1 nan
68818964 104392 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 427 5 2 6 2.3 N[C@H](COc1cccc2c1NC(=O)CO2)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
CHEMBL3099958 104392 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis
ChEMBL 427 5 2 6 2.3 N[C@H](COc1cccc2c1NC(=O)CO2)CN1CCC2(CC1)Cc1cc(F)ccc1O2 10.1016/j.bmcl.2013.11.062
12425 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
1318 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
CHEMBL415879 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
DB02365 6 None 76 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrsDisplacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs
ChEMBL 180 0 0 2 2.8 C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 10.1021/jm301121j
12112109 145275 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 491 8 3 5 3.1 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2NC(=O)NCCN)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL391238 145275 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 491 8 3 5 3.1 C[C@H]1CN(C(=O)COc2ccc(Cl)cc2NC(=O)NCCN)[C@H](C)CN1Cc1ccc(F)cc1 10.1016/j.bmcl.2007.03.037
57840435 86890 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 424 5 0 5 4.0 COc1cc(N2CCN(C(=O)Cn3nc(C(C)C)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322844 86890 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 424 5 0 5 4.0 COc1cc(N2CCN(C(=O)Cn3nc(C(C)C)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
58778003 86906 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 494 4 0 5 4.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Br)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322859 86906 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 494 4 0 5 4.0 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Br)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
24758295 82872 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 418 6 1 2 5.2 CC(C)[C@@H](NC(=O)CC1CCCCC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180505 82872 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 418 6 1 2 5.2 CC(C)[C@@H](NC(=O)CC1CCCCC1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44309312 206236 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 460 9 3 5 3.4 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCCC1 10.1016/j.bmcl.2004.02.022
CHEMBL68145 206236 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 460 9 3 5 3.4 NC(=O)C(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCCC1 10.1016/j.bmcl.2004.02.022
44309337 206418 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 460 9 3 5 3.4 NC(=O)[C@@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCCC1 10.1016/j.bmcl.2004.02.021
CHEMBL69375 206418 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 460 9 3 5 3.4 NC(=O)[C@@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C1CCCCC1 10.1016/j.bmcl.2004.02.021
71680936 91213 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 563 8 3 6 3.2 CC(C)[C@@H](NC(=O)C1CCCC1(O)CCN1CCOCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398750 91213 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 563 8 3 6 3.2 CC(C)[C@@H](NC(=O)C1CCCC1(O)CCN1CCOCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
10254761 90814 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 484 6 2 6 2.6 Cc1ccc(C(=O)N2CC[C@H](O)C2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(F)ccc2O3)c1 10.1016/j.bmcl.2013.04.047
CHEMBL2391798 90814 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 484 6 2 6 2.6 Cc1ccc(C(=O)N2CC[C@H](O)C2)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(F)ccc2O3)c1 10.1016/j.bmcl.2013.04.047
57889649 91196 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 486 6 3 4 3.9 CC(C)[C@@H](NC(=O)c1cccc(C(=O)O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398733 91196 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 486 6 3 4 3.9 CC(C)[C@@H](NC(=O)c1cccc(C(=O)O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
24759420 82880 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 448 5 1 2 5.7 CC(C)C(NC(=O)c1ccc2ccccc2c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180513 82880 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 448 5 1 2 5.7 CC(C)C(NC(=O)c1ccc2ccccc2c1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44453403 95189 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2007.09.068
CHEMBL255629 95189 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.3 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2007.09.068
44430736 153563 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 576 10 2 7 4.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2ccccc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL397956 153563 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 576 10 2 7 4.5 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCc2ccccc2)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453263 155731 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL404732 155731 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 442 7 2 4 3.6 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.068
10695296 99897 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 460 4 1 3 6.6 O=C(NC1CCN(CC2CCCCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1016/j.ejmech.2020.113085
CHEMBL285703 99897 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assayInhibition of human CCR1 transfected in CHO cells incubated for 1 hr in presence of 125I-chemokine by radioactivity based assay
ChEMBL 460 4 1 3 6.6 O=C(NC1CCN(CC2CCCCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1016/j.ejmech.2020.113085
10816699 11180 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 433 6 1 1 5.9 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm0004244
CHEMBL1178593 11180 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 433 6 1 1 5.9 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm0004244
CHEMBL33761 11180 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 433 6 1 1 5.9 C[N+]1(CC2CCCCCCC2)CCC(NC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm0004244
10695296 99897 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 460 4 1 3 6.6 O=C(NC1CCN(CC2CCCCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
CHEMBL285703 99897 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 460 4 1 3 6.6 O=C(NC1CCN(CC2CCCCCCCCC2)CC1)C1c2ccccc2Oc2ccccc21 10.1021/jm0004244
44309091 206199 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 439 10 3 4 4.2 CC(C)C[C@H](C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1)C(N)=O 10.1016/j.bmcl.2004.02.020
CHEMBL67809 206199 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 439 10 3 4 4.2 CC(C)C[C@H](C[C@H](O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2c1)C(N)=O 10.1016/j.bmcl.2004.02.020
59444207 171941 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 470 7 2 3 4.4 CC(C)[C@@H](CNC(=O)Cc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL4468705 171941 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 470 7 2 3 4.4 CC(C)[C@@H](CNC(=O)Cc1ccccc1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
49865901 16193 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 463 4 1 4 5.7 Cc1nc([C@H]2CCCN2C(=O)Nc2ccc(C(F)(F)F)cc2)n(Cc2ccc(Cl)cc2)n1 10.1016/j.bmcl.2010.07.082
CHEMBL1224121 16193 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPADisplacement of [125I]-MIP1-alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPA
ChEMBL 463 4 1 4 5.7 Cc1nc([C@H]2CCCN2C(=O)Nc2ccc(C(F)(F)F)cc2)n(Cc2ccc(Cl)cc2)n1 10.1016/j.bmcl.2010.07.082
59474969 130347 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 482 4 2 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@@]2(C)NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679658 130347 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 482 4 2 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@@]2(C)NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
59474969 130347 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 482 4 2 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@@]2(C)NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679658 130347 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 482 4 2 3 5.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@@]2(C)NC(=O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
24758745 82865 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 7 1 2 4.6 CC[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180498 82865 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 7 1 2 4.6 CC[C@@H](NC(=O)CCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44309245 205902 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 556 13 3 5 5.2 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.02.022
CHEMBL65784 205902 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 556 13 3 5 5.2 CC(C)(F)CCC(C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.02.022
57888886 82896 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 444 6 2 4 4.1 CC(C)C(NC(=O)OCc1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180529 82896 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 444 6 2 4 4.1 CC(C)C(NC(=O)OCc1ccccc1)C(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
25174629 130337 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679648 130337 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174629 130337 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679648 130337 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 498 5 3 4 4.2 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)[C@H](O)c2ccccc2)CC[C@]1(O)c1ccc(Cl)cc1 nan
9999626 88099 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 376 5 0 3 3.6 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1 10.1016/j.bmcl.2007.03.037
CHEMBL234622 88099 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Affinity at CCL3Binding Affinity at CCL3
ChEMBL 376 5 0 3 3.6 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1 10.1016/j.bmcl.2007.03.037
57889944 82910 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 6 1 2 5.2 Cc1ccccc1C(=O)NC(CC(C)C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180543 82910 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 426 6 1 2 5.2 Cc1ccccc1C(=O)NC(CC(C)C)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
68963698 90823 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 543 7 3 7 2.6 CC(=O)N[C@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
CHEMBL2391807 90823 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
ChEMBL 543 7 3 7 2.6 CC(=O)N[C@H]1CCN(C(=O)c2ccc(O)cc2OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)C1 10.1016/j.bmcl.2013.04.047
44453467 95785 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL258359 95785 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 502 4 1 4 4.8 O=S(=O)(c1ccccc1Cl)N1CCC(N2CCC(O)(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.09.068
10985078 114802 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm0201767
CHEMBL333865 114802 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cellsInhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
ChEMBL 635 10 3 3 8.2 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm0201767
57889635 114540 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 435 4 2 3 3.6 CC(C)[C@@H](NC(=O)N1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
CHEMBL3334819 114540 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 435 4 2 3 3.6 CC(C)[C@@H](NC(=O)N1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1021/jm5003167
68818375 87391 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 443 7 2 6 3.0 COc1ccc(NC(C)=O)c(OC[C@@H](N)CN2CCC3(CC2)Cc2cc(F)ccc2O3)c1 10.1016/j.bmcl.2012.12.095
CHEMBL2332938 87391 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs
ChEMBL 443 7 2 6 3.0 COc1ccc(NC(C)=O)c(OC[C@@H](N)CN2CCC3(CC2)Cc2cc(F)ccc2O3)c1 10.1016/j.bmcl.2012.12.095
44309397 206267 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 466 11 3 5 3.4 CC(C)(F)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
CHEMBL68366 206267 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCL3 binding to C-C chemokine receptor type 1Inhibition of CCL3 binding to C-C chemokine receptor type 1
ChEMBL 466 11 3 5 3.4 CC(C)(F)CC[C@H](C[C@H](O)[C@H](Cc1ccccc1)NC(=O)c1cnc2ccccc2n1)C(N)=O 10.1016/j.bmcl.2004.02.022
52916803 171085 None 20 Human Binding pIC50 = 8.1 8.1 - 1
Receptor internalizationReceptor internalization
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
CHEMBL4456123 171085 None 20 Human Binding pIC50 = 8.1 8.1 - 1
Receptor internalizationReceptor internalization
ChEMBL 451 5 1 7 2.8 CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1 10.6019/CHEMBL4507278
44537841 675 None 16 Human Binding pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57889181 675 None 16 Human Binding pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
9497 675 None 16 Human Binding pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL2398716 675 None 16 Human Binding pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
CHEMBL3334824 675 None 16 Human Binding pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 minsAntagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 mins
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 10.1021/jm5003167
57888707 91228 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 413 6 1 3 3.8 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
CHEMBL2398768 91228 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 413 6 1 3 3.8 CC(C)[C@@H](NC(=O)Cc1ccncc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.04.079
10555551 11174 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 473 6 1 2 6.6 C=CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL1178575 11174 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 473 6 1 2 6.6 C=CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
CHEMBL33104 11174 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
ChEMBL 473 6 1 2 6.6 C=CC[N+]1(CC2CCCCCCC2)CCC(NC(=O)C2c3ccccc3Oc3ccccc32)CC1 10.1021/jm0004244
57888900 91227 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 521 6 3 5 2.9 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398767 91227 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxisAntagonist activity at human CCR1 assessed as inhibition of MIP1alpha-induced chemotaxis
ChEMBL 521 6 3 5 2.9 CC(C)[C@@H](NC(=O)c1cccc(S(N)(=O)=O)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
57888966 91231 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1cccc(Cl)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
CHEMBL2398771 91231 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to human CCR1Binding affinity to human CCR1
ChEMBL 476 5 2 3 4.9 CC(C)[C@@H](NC(=O)c1cccc(Cl)c1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 10.1016/j.bmcl.2013.04.079
44430725 167866 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 480 8 2 7 2.6 CNc1c(Nc2cc(C)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL430356 167866 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 480 8 2 7 2.6 CNc1c(Nc2cc(C)ccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
25022507 155515 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL403728 155515 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 512 4 1 4 4.2 O=S(=O)(c1ccccc1Br)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
44453361 167419 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 456 7 2 4 4.0 Cc1cccc(Cl)c1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL429419 167419 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 456 7 2 4 4.0 Cc1cccc(Cl)c1S(=O)(=O)NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.068
21070989 86923 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at CCR1 in mouse WEHI274.1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxisAntagonist activity at CCR1 in mouse WEHI274.1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322875 86923 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at CCR1 in mouse WEHI274.1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxisAntagonist activity at CCR1 in mouse WEHI274.1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxis
ChEMBL 450 4 0 5 3.9 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44453165 95788 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL258362 95788 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 492 8 2 5 3.9 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
44453229 95452 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL256889 95452 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 426 7 2 4 3.1 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2007.09.068
57840460 86902 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)C[C@H]2C)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322855 86902 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 464 4 0 5 4.3 COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)C[C@H]2C)ccc1Cl 10.1016/j.bmcl.2013.01.005
44430722 86874 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 466 8 2 7 2.3 CNc1c(Nc2ccccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232252 86874 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 466 8 2 7 2.3 CNc1c(Nc2ccccc2OCC(=O)N2CCN(Cc3ccc(F)cc3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
1370410 86936 None 9 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxis
ChEMBL 404 3 0 4 3.4 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322888 86936 None 9 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3/MIP-1alpha-induced chemotaxis
ChEMBL 404 3 0 4 3.4 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2013.01.005
25174306 130334 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 503 6 2 4 4.3 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCN2CCCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679645 130334 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 503 6 2 4 4.3 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCN2CCCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
25174306 130334 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 503 6 2 4 4.3 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCN2CCCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
CHEMBL3679645 130334 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 503 6 2 4 4.3 CC1(C)CN(C(=O)[C@H]2CCCC[C@H]2NC(=O)CCN2CCCCC2)CC[C@]1(O)c1ccc(Cl)cc1 nan
57889234 82897 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 2 3 3.1 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(F)cc2)CC1 10.1021/jm300896d
CHEMBL2180530 82897 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 398 5 2 3 3.1 CC(C)C(NC(=O)c1ccccc1)C(=O)N1CCC(O)(c2ccc(F)cc2)CC1 10.1021/jm300896d
44453167 95789 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
CHEMBL258363 95789 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 476 7 2 4 4.0 O=S(=O)(NCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.09.068
57991690 82883 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 8 1 2 5.2 CC(C)[C@@H](NC(=O)CCCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
CHEMBL2180516 82883 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 440 8 1 2 5.2 CC(C)[C@@H](NC(=O)CCCc1ccccc1)C(=O)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm300896d
44430746 87151 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232638 87151 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 530 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCO)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44430748 87255 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232837 87255 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Binding affinity at mouse CCR1Binding affinity at mouse CCR1
ChEMBL 529 10 3 8 2.3 C[C@@H]1CN(Cc2ccc(F)cc2)CCN1C(=O)COc1ccc(Cl)cc1Nc1c(NCCN)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
57840315 86895 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 6 2.3 COc1cc(N2CCN(C(=O)Cn3nc(CO)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
CHEMBL2322849 86895 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 412 5 1 6 2.3 COc1cc(N2CCN(C(=O)Cn3nc(CO)c(Cl)c3C)CC2)ccc1Cl 10.1016/j.bmcl.2013.01.005
44430717 86794 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 518 8 2 7 3.1 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)c(F)c3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
CHEMBL232043 86794 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 expressed in THP1 cells
ChEMBL 518 8 2 7 3.1 CNc1c(Nc2cc(Cl)ccc2OCC(=O)N2CCN(Cc3ccc(F)c(F)c3)C[C@H]2C)c(=O)c1=O 10.1016/j.bmcl.2007.03.104
44453225 95791 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 440 4 1 5 3.5 O=S(=O)(c1cccs1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
CHEMBL258368 95791 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cellsDisplacement of [125I]MIP1-alpha from human CCR1 receptor expressed in THP1 cells
ChEMBL 440 4 1 5 3.5 O=S(=O)(c1cccs1)N1CCC(N2CCC(O)(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.09.068
21071094 86938 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 420 3 0 4 3.9 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2322890 86938 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 420 3 0 4 3.9 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.01.005
21071099 86982 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 454 3 0 4 4.2 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2013.01.005
CHEMBL2323419 86982 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cellsDisplacement of [125I]-CCL3/MIP-1alpha from CCR1 in human THP1 cells
ChEMBL 454 3 0 4 4.2 Cc1c(Cl)c(C(F)(F)F)nn1CC(=O)N1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2013.01.005
59444200 173294 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 514 7 2 5 4.6 CCOC(=O)c1cc(C2(O)CCN(C(=O)CC(C)(C)NC(=O)c3ccccc3)CC2(C)C)ccc1Cl nan
CHEMBL4522473 173294 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP-1 cells after 12 h by scintillation proximity assay
ChEMBL 514 7 2 5 4.6 CCOC(=O)c1cc(C2(O)CCN(C(=O)CC(C)(C)NC(=O)c3ccccc3)CC2(C)C)ccc1Cl nan
25176401 130332 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 422 3 2 4 3.7 COC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL3679643 130332 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay
ChEMBL 422 3 2 4 3.7 COC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
25176401 130332 None 0 Human Binding pIC50 = 6 6.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 422 3 2 4 3.7 COC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL3679643 130332 None 0 Human Binding pIC50 = 6 6.0 - 0
Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).
ChEMBL 422 3 2 4 3.7 COC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
512282 758 None 42 Human Binding pKd = 9 9.0 147 2
Binding affinity to human CCR1 by radioligand binding assayBinding affinity to human CCR1 by radioligand binding assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
767 758 None 42 Human Binding pKd = 9 9.0 147 2
Binding affinity to human CCR1 by radioligand binding assayBinding affinity to human CCR1 by radioligand binding assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
CHEMBL232656 758 None 42 Human Binding pKd = 9 9.0 147 2
Binding affinity to human CCR1 by radioligand binding assayBinding affinity to human CCR1 by radioligand binding assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
512282 758 None 42 Mouse Binding pKd = 6.7 6.7 -147 2
Binding affinity to mouse CCR1 by radioligand binding assayBinding affinity to mouse CCR1 by radioligand binding assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
767 758 None 42 Mouse Binding pKd = 6.7 6.7 -147 2
Binding affinity to mouse CCR1 by radioligand binding assayBinding affinity to mouse CCR1 by radioligand binding assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
CHEMBL232656 758 None 42 Mouse Binding pKd = 6.7 6.7 -147 2
Binding affinity to mouse CCR1 by radioligand binding assayBinding affinity to mouse CCR1 by radioligand binding assay
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
25109291 191495 None 6 Human Binding pKi = 10.4 10.4 56 12
Displacement of radiolabeled MIP1alpha from human CCR1 receptorDisplacement of radiolabeled MIP1alpha from human CCR1 receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 191495 None 6 Human Binding pKi = 10.4 10.4 56 12
Displacement of radiolabeled MIP1alpha from human CCR1 receptorDisplacement of radiolabeled MIP1alpha from human CCR1 receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
57889392 127130 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 423 5 3 3 3.5 CC(C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C nan
CHEMBL3656279 127130 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 423 5 3 3 3.5 CC(C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C nan
57889423 91210 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 434 5 2 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
CHEMBL2398747 91210 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 434 5 2 3 4.1 CC(C)[C@@H](NC(=O)C1CCCC1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 nan
512282 758 None 42 Human Binding pKi = 9 9.0 147 2
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
767 758 None 42 Human Binding pKi = 9 9.0 147 2
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
CHEMBL232656 758 None 42 Human Binding pKi = 9 9.0 147 2
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10.1021/jm300682j
10371087 82600 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 584 6 2 5 6.0 NCC1CCCN(C(=O)c2ccc3c(c2)C(C(=O)NC2CCN(C/C4=C/CCCCCCC4)CC2)c2ccccc2O3)C1 10.1021/jm300682j
CHEMBL2178571 82600 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 584 6 2 5 6.0 NCC1CCCN(C(=O)c2ccc3c(c2)C(C(=O)NC2CCN(C/C4=C/CCCCCCC4)CC2)c2ccccc2O3)C1 10.1021/jm300682j
10111333 175571 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175571 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
71461438 84010 None 0 Human Binding pKi = 6 6.0 -100 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207082 84010 None 0 Human Binding pKi = 6 6.0 -100 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214725 84011 None 0 Human Binding pKi = 6 6.0 -25 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207083 84011 None 0 Human Binding pKi = 6 6.0 -25 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461439 84015 None 0 Human Binding pKi = 6 6.0 -10 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207087 84015 None 0 Human Binding pKi = 6 6.0 -10 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
71452488 84021 None 0 Human Binding pKi = 6 6.0 -19 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207093 84021 None 0 Human Binding pKi = 6 6.0 -19 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
71461440 84025 None 0 Human Binding pKi = 6 6.0 -31 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207097 84025 None 0 Human Binding pKi = 6 6.0 -31 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15604497 84027 None 0 Human Binding pKi = 6 6.0 -39 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207099 84027 None 0 Human Binding pKi = 6 6.0 -39 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10809142 35377 None 0 Human Binding pKi = 6 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 369 6 1 4 4.1 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccnc1 10.1021/jm990316l
CHEMBL143741 35377 None 0 Human Binding pKi = 6 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 369 6 1 4 4.1 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccnc1 10.1021/jm990316l
68557448 170324 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 417 5 1 5 4.2 COc1cccc(N2CCC(C(O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c1 nan
CHEMBL4445508 170324 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 417 5 1 5 4.2 COc1cccc(N2CCC(C(O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c1 nan
10788075 119477 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 416 7 1 4 5.3 N#CC(CCCN1CCC(O)(c2cccs2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL344751 119477 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 416 7 1 4 5.3 N#CC(CCCN1CCC(O)(c2cccs2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
10111333 175571 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175571 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155568814 176169 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 403 5 1 5 3.8 COc1cc(N2CCC(C(O)Cn3ccc(C(F)(F)F)n3)CC2)ccc1Cl nan
CHEMBL4590794 176169 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 403 5 1 5 3.8 COc1cc(N2CCC(C(O)Cn3ccc(C(F)(F)F)n3)CC2)ccc1Cl nan
10599794 34223 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 453 8 1 4 5.3 CN(C)c1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
CHEMBL142628 34223 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 453 8 1 4 5.3 CN(C)c1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
10526132 72502 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 419 7 1 2 6.2 OC1(c2ccc(Cl)cc2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
CHEMBL142004 72502 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 419 7 1 2 6.2 OC1(c2ccc(Cl)cc2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
CHEMBL198935 72502 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 419 7 1 2 6.2 OC1(c2ccc(Cl)cc2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
44362079 119236 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 422 5 1 3 5.2 N#CC1(CCCN2CCC(O)(c3ccccc3)CC2)c2ccccc2Cc2ccccc21 10.1021/jm990316l
CHEMBL343032 119236 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 422 5 1 3 5.2 N#CC1(CCCN2CCC(O)(c3ccccc3)CC2)c2ccccc2Cc2ccccc21 10.1021/jm990316l
24863547 174819 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 484 5 1 5 5.4 COc1cc(N2CCC(C(N)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c(Cl)cc1Cl nan
CHEMBL4559982 174819 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 484 5 1 5 5.4 COc1cc(N2CCC(C(N)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)c(Cl)cc1Cl nan
10811393 34895 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 407 7 1 4 4.8 N#CCC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL143194 34895 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 407 7 1 4 4.8 N#CCC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
24863719 175976 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 465 5 1 5 5.2 COc1cc(N2CCC(C)(C(O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl nan
CHEMBL4586066 175976 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 465 5 1 5 5.2 COc1cc(N2CCC(C)(C(O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl nan
71214976 84030 None 0 Human Binding pKi = 5.9 5.9 -100 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207101 84030 None 0 Human Binding pKi = 5.9 5.9 -100 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
10547456 119650 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1021/jm990316l
CHEMBL346205 119650 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccs1 10.1021/jm990316l
10503785 121183 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 451 7 1 4 5.3 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)N1CCCCC1 10.1021/jm990316l
CHEMBL357434 121183 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 451 7 1 4 5.3 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)N1CCCCC1 10.1021/jm990316l
10528677 168635 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 478 7 1 3 6.6 N#CC(CCCN1CCC(O)(c2cc(Cl)cc(Cl)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL435480 168635 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 478 7 1 3 6.6 N#CC(CCCN1CCC(O)(c2cc(Cl)cc(Cl)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
10812461 78878 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 428 7 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(F)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL2112832 78878 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 428 7 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(F)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
10133557 172642 None 0 Human Binding pKi = 6.9 6.9 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 172642 None 0 Human Binding pKi = 6.9 6.9 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10645391 33592 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 412 8 1 4 5.1 CCOc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990316l
CHEMBL142107 33592 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 412 8 1 4 5.1 CCOc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990316l
10133557 172642 None 0 Human Binding pKi = 6.8 6.8 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 172642 None 0 Human Binding pKi = 6.8 6.8 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
68552829 171414 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 473 7 2 6 3.2 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)cc3C)NC(=O)CN)CC2)ccc1Cl nan
CHEMBL4461035 171414 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 473 7 2 6 3.2 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)cc3C)NC(=O)CN)CC2)ccc1Cl nan
12093167 172428 None 31 Human Binding pKi = 7.8 7.8 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 172428 None 31 Human Binding pKi = 7.8 7.8 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
12093167 172428 None 31 Human Binding pKi = 7.8 7.8 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 172428 None 31 Human Binding pKi = 7.8 7.8 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10743274 119379 None 0 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 478 7 1 3 6.3 N#CC(CCCN1CCC(O)(c2ccc(C(F)(F)F)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL344075 119379 None 0 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 478 7 1 3 6.3 N#CC(CCCN1CCC(O)(c2ccc(C(F)(F)F)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
68551780 174250 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 418 5 1 6 3.5 COc1cc(N2CCC(C(O)Cn3nc(C(F)(F)F)nc3C)CC2)ccc1Cl nan
CHEMBL4546480 174250 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 418 5 1 6 3.5 COc1cc(N2CCC(C(O)Cn3nc(C(F)(F)F)nc3C)CC2)ccc1Cl nan
10833944 118820 None 0 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(O)c1 10.1021/jm990316l
CHEMBL341840 118820 None 0 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(O)c1 10.1021/jm990316l
71214710 84013 None 0 Human Binding pKi = 5.8 5.8 -100 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207085 84013 None 0 Human Binding pKi = 5.8 5.8 -100 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71452487 84016 None 0 Human Binding pKi = 5.8 5.8 -15 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207088 84016 None 0 Human Binding pKi = 5.8 5.8 -15 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
71454247 84018 None 0 Human Binding pKi = 5.8 5.8 -15 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207090 84018 None 0 Human Binding pKi = 5.8 5.8 -15 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
71456008 84023 None 0 Human Binding pKi = 5.8 5.8 -25 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207095 84023 None 0 Human Binding pKi = 5.8 5.8 -25 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
3798520 170549 None 6 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 307 3 1 3 3.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4448679 170549 None 6 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 307 3 1 3 3.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccccc1 10.1021/acs.jmedchem.8b00605
3798520 170549 None 6 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 307 3 1 3 3.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4448679 170549 None 6 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 307 3 1 3 3.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccccc1 10.1021/acs.jmedchem.8b00605
3063068 33266 None 1 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 468 5 1 4 6.2 Cc1ccccc1C1(O)CCN(CCCC2(C#N)c3ccccc3CSc3ccccc32)CC1 10.1021/jm990316l
CHEMBL141829 33266 None 1 Human Binding pKi = 6.8 6.8 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 468 5 1 4 6.2 Cc1ccccc1C1(O)CCN(CCCC2(C#N)c3ccccc3CSc3ccccc32)CC1 10.1021/jm990316l
9967166 170076 None 8 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 170076 None 8 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
9967166 170076 None 8 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 170076 None 8 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155535265 172122 None 0 Human Binding pKi = 7.7 7.7 8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 172122 None 0 Human Binding pKi = 7.7 7.7 8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155532102 171831 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4467095 171831 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
155532102 171831 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4467095 171831 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
155535265 172122 None 0 Human Binding pKi = 7.7 7.7 8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 172122 None 0 Human Binding pKi = 7.7 7.7 8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155561022 175079 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 321 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(C)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4566226 175079 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 321 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(C)cc1 10.1021/acs.jmedchem.8b00605
155553428 174293 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Cl)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4547735 174293 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Cl)c1 10.1021/acs.jmedchem.8b00605
155561022 175079 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 321 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(C)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4566226 175079 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 321 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(C)cc1 10.1021/acs.jmedchem.8b00605
54712652 170086 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 343 4 1 4 3.7 CCOC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4442093 170086 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 343 4 1 4 3.7 CCOC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155553428 174293 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Cl)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4547735 174293 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1cccc(Cl)c1 10.1021/acs.jmedchem.8b00605
71463166 84024 None 0 Human Binding pKi = 5.7 5.7 -7 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207096 84024 None 0 Human Binding pKi = 5.7 5.7 -7 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
57889188 114537 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 437 6 3 3 3.9 CC[C@@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C nan
CHEMBL3334816 114537 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 437 6 3 3 3.9 CC[C@@H](C)NC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C nan
71462570 82598 None 0 Human Binding pKi = 8.6 8.6 -2 3
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 518 5 2 5 5.6 CC1(C)CN(CC/C=C2/c3cc(C(=O)O)ccc3OCc3ncccc32)C[C@H](c2ccc(Cl)cc2)[C@H]1O 10.1021/jm300682j
CHEMBL2178569 82598 None 0 Human Binding pKi = 8.6 8.6 -2 3
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 518 5 2 5 5.6 CC1(C)CN(CC/C=C2/c3cc(C(=O)O)ccc3OCc3ncccc32)C[C@H](c2ccc(Cl)cc2)[C@H]1O 10.1021/jm300682j
57889334 91206 None 0 Human Binding pKi = 8.6 8.6 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 422 6 2 3 4.0 CC(C)CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C nan
CHEMBL2398743 91206 None 0 Human Binding pKi = 8.6 8.6 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 422 6 2 3 4.0 CC(C)CC(=O)N[C@@H](C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)C nan
54712652 170086 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 343 4 1 4 3.7 CCOC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4442093 170086 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 343 4 1 4 3.7 CCOC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
3063066 33757 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 454 5 1 4 5.9 N#CC1(CCCN2CCC(O)(c3ccccc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL142244 33757 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 454 5 1 4 5.9 N#CC1(CCCN2CCC(O)(c3ccccc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
10695080 12206 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 418 6 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1021/jm990316l
CHEMBL1184276 12206 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 418 6 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1021/jm990316l
CHEMBL342444 12206 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 418 6 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1021/jm990316l
10645313 32306 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 411 7 1 4 4.7 N#CC(CCCN1CCC(O)(c2cccnc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL141020 32306 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 411 7 1 4 4.7 N#CC(CCCN1CCC(O)(c2cccnc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
10132885 175242 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 175242 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
10132885 175242 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 175242 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
10076510 11643 None 0 Human Binding pKi = 7.7 7.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 433 6 1 2 6.0 C[N+]1(CCCC(C#N)c2ccc3ccccc3c2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL1180795 11643 None 0 Human Binding pKi = 7.7 7.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 433 6 1 2 6.0 C[N+]1(CCCC(C#N)c2ccc3ccccc3c2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL143374 11643 None 0 Human Binding pKi = 7.7 7.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 433 6 1 2 6.0 C[N+]1(CCCC(C#N)c2ccc3ccccc3c2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
9850002 35089 None 0 Human Binding pKi = 7.7 7.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 532 5 1 4 6.6 N#CC1(CCCN2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL143350 35089 None 0 Human Binding pKi = 7.7 7.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 532 5 1 4 6.6 N#CC1(CCCN2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
68556971 170586 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 474 7 2 6 3.3 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)cc3C)NC(=O)CO)CC2)ccc1Cl nan
CHEMBL4449145 170586 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 474 7 2 6 3.3 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)cc3C)NC(=O)CO)CC2)ccc1Cl nan
68556936 172436 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 401 5 2 7 3.0 COc1cc(N2CCC(C(O)Cn3nc(N)c4cccnc43)CC2)ccc1Cl nan
CHEMBL4475524 172436 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 401 5 2 7 3.0 COc1cc(N2CCC(C(O)Cn3nc(N)c4cccnc43)CC2)ccc1Cl nan
10530837 35459 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 556 5 1 4 7.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL143814 35459 None 0 Human Binding pKi = 6.7 6.7 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 556 5 1 4 7.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
10293022 171201 None 8 Human Binding pKi = 7.6 7.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 171201 None 8 Human Binding pKi = 7.6 7.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10554359 34283 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 536 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(I)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL142676 34283 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 536 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(I)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
10766333 35147 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 5 1 4 6.0 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2Oc2ccccc21 10.1021/jm990316l
CHEMBL143449 35147 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 5 1 4 6.0 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2Oc2ccccc21 10.1021/jm990316l
10690854 32756 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1021/jm990316l
CHEMBL141387 32756 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 374 6 1 4 4.8 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccsc1 10.1021/jm990316l
10293022 171201 None 8 Human Binding pKi = 7.6 7.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 171201 None 8 Human Binding pKi = 7.6 7.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
5311125 35181 None 0 Human Binding pKi = 7.6 7.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 488 5 1 4 6.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL143492 35181 None 0 Human Binding pKi = 7.6 7.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 488 5 1 4 6.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
10623381 16909 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 448 8 2 3 5.3 NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL125111 16909 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 448 8 2 3 5.3 NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
12093162 173430 None 0 Human Binding pKi = 6.6 6.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 173430 None 0 Human Binding pKi = 6.6 6.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
71457815 84019 None 0 Human Binding pKi = 5.6 5.6 -50 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207091 84019 None 0 Human Binding pKi = 5.6 5.6 -50 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
12093162 173430 None 0 Human Binding pKi = 6.6 6.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 173430 None 0 Human Binding pKi = 6.6 6.6 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
9967349 173168 None 0 Human Binding pKi = 7.6 7.6 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 173168 None 0 Human Binding pKi = 7.6 7.6 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155559153 174885 None 0 Human Binding pKi = 7.6 7.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174885 None 0 Human Binding pKi = 7.6 7.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
155559153 174885 None 0 Human Binding pKi = 7.6 7.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174885 None 0 Human Binding pKi = 7.6 7.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
9902578 171458 None 0 Human Binding pKi = 7.5 7.5 4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 171458 None 0 Human Binding pKi = 7.5 7.5 4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9902578 171458 None 0 Human Binding pKi = 7.5 7.5 4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 171458 None 0 Human Binding pKi = 7.5 7.5 4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967349 173168 None 0 Human Binding pKi = 7.5 7.5 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 173168 None 0 Human Binding pKi = 7.5 7.5 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
44361881 168636 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 500 5 1 3 5.9 N#CC1(CCCN2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc2Cc2ccccc21 10.1021/jm990316l
CHEMBL435485 168636 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 500 5 1 3 5.9 N#CC1(CCCN2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc2Cc2ccccc21 10.1021/jm990316l
24764465 175878 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 556 7 2 6 5.0 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(=O)[C@@H](C)O)CC2)c(Cl)cc1Cl nan
CHEMBL4583778 175878 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 556 7 2 6 5.0 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(=O)[C@@H](C)O)CC2)c(Cl)cc1Cl nan
44537841 675 None 16 Human Binding pKi = 8.4 8.4 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C nan
57889181 675 None 16 Human Binding pKi = 8.4 8.4 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C nan
9497 675 None 16 Human Binding pKi = 8.4 8.4 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C nan
CHEMBL2398716 675 None 16 Human Binding pKi = 8.4 8.4 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C nan
CHEMBL3334824 675 None 16 Human Binding pKi = 8.4 8.4 - 1
Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.
ChEMBL 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C nan
155539148 172907 None 0 Human Binding pKi = 7.5 7.5 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172907 None 0 Human Binding pKi = 7.5 7.5 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155539148 172907 None 0 Human Binding pKi = 7.5 7.5 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172907 None 0 Human Binding pKi = 7.5 7.5 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
22725647 173803 None 0 Human Binding pKi = 7.5 7.5 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173803 None 0 Human Binding pKi = 7.5 7.5 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10501338 121107 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 402 6 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Cl 10.1021/jm990316l
CHEMBL356764 121107 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 402 6 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Cl 10.1021/jm990316l
155545804 173601 None 0 Human Binding pKi = 7.5 7.5 5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 173601 None 0 Human Binding pKi = 7.5 7.5 5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
22725647 173803 None 0 Human Binding pKi = 7.5 7.5 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173803 None 0 Human Binding pKi = 7.5 7.5 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155545804 173601 None 0 Human Binding pKi = 7.5 7.5 5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 173601 None 0 Human Binding pKi = 7.5 7.5 5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
71450658 84026 None 0 Human Binding pKi = 6.5 6.5 -31 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207098 84026 None 0 Human Binding pKi = 6.5 6.5 -31 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71454248 84029 None 0 Human Binding pKi = 6.5 6.5 -25 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207100 84029 None 0 Human Binding pKi = 6.5 6.5 -25 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
10649043 34563 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 499 5 1 4 5.5 CN1C(=O)c2ccccc2C(C#N)(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1021/jm990316l
CHEMBL142925 34563 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 499 5 1 4 5.5 CN1C(=O)c2ccccc2C(C#N)(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1021/jm990316l
10717972 119415 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 440 8 1 5 4.4 CCOC(=O)C(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL344324 119415 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 440 8 1 5 4.4 CCOC(=O)C(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
10647579 35401 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 6 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1c(F)c(F)c(F)c(F)c1F 10.1021/jm990316l
CHEMBL143772 35401 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 6 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1c(F)c(F)c(F)c(F)c1F 10.1021/jm990316l
9956488 119302 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 472 5 1 4 5.8 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2COc2ccccc21 10.1021/jm990316l
CHEMBL343511 119302 None 0 Human Binding pKi = 7.5 7.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 472 5 1 4 5.8 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2COc2ccccc21 10.1021/jm990316l
10672205 119443 None 0 Human Binding pKi = 5.5 5.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 474 9 1 4 6.3 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(OCc2ccccc2)cc1 10.1021/jm990316l
CHEMBL344499 119443 None 0 Human Binding pKi = 5.5 5.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 474 9 1 4 6.3 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(OCc2ccccc2)cc1 10.1021/jm990316l
10670785 33128 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 440 8 1 4 5.3 COc1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
CHEMBL141713 33128 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 440 8 1 4 5.3 COc1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
44199443 170642 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 378 6 2 3 4.0 CCC(NC(=O)C1CCCC1)C(O)C1CCN(c2ccc(Cl)cc2)CC1 nan
CHEMBL4449875 170642 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 378 6 2 3 4.0 CCC(NC(=O)C1CCCC1)C(O)C1CCN(c2ccc(Cl)cc2)CC1 nan
10597049 33249 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 398 7 1 4 4.7 COc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990316l
CHEMBL141817 33249 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 398 7 1 4 4.7 COc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990316l
10837160 121186 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 446 6 1 3 5.5 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Br 10.1021/jm990316l
CHEMBL357445 121186 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 446 6 1 3 5.5 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1Br 10.1021/jm990316l
10596333 33660 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 386 6 1 3 4.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1F 10.1021/jm990316l
CHEMBL142160 33660 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 386 6 1 3 4.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1F 10.1021/jm990316l
9902204 170229 None 8 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 170229 None 8 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10503474 34317 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2cccc(Cl)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL142713 34317 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2cccc(Cl)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
15985912 84009 None 0 Human Binding pKi = 6.4 6.4 -2 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 84009 None 0 Human Binding pKi = 6.4 6.4 -2 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 84012 None 0 Human Binding pKi = 6.4 6.4 -14 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 84012 None 0 Human Binding pKi = 6.4 6.4 -14 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71454246 84017 None 0 Human Binding pKi = 5.4 5.4 -7 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
CHEMBL2207089 84017 None 0 Human Binding pKi = 5.4 5.4 -7 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
87494453 175061 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 544 7 1 5 5.6 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(=O)CF)CC2)c(Cl)cc1Cl nan
CHEMBL4565880 175061 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 544 7 1 5 5.6 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(=O)CF)CC2)c(Cl)cc1Cl nan
9902204 170229 None 8 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 170229 None 8 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155513751 169904 None 0 Human Binding pKi = 7.4 7.4 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169904 None 0 Human Binding pKi = 7.4 7.4 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
10694874 34979 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 450 7 1 3 6.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)C1CCCCC1 10.1021/jm990316l
CHEMBL143266 34979 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 450 7 1 3 6.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)C1CCCCC1 10.1021/jm990316l
10524463 164980 None 0 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 390 9 1 3 5.3 CCCCC1(O)CCN(CCCC(C#N)(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
CHEMBL422115 164980 None 0 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 390 9 1 3 5.3 CCCCC1(O)CCN(CCCC(C#N)(c2ccccc2)c2ccccc2)CC1 10.1021/jm990316l
10838033 119158 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 468 6 1 4 6.0 N#CC1(CCCN2CCC(O)(Cc3ccccc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL342721 119158 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 468 6 1 4 6.0 N#CC1(CCCN2CCC(O)(Cc3ccccc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
10814504 121103 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.6 COC(=O)C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL356718 121103 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.6 COC(=O)C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
9845614 121346 None 19 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 430 6 1 3 5.5 N#CC(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL357919 121346 None 19 Human Binding pKi = 5.4 5.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 430 6 1 3 5.5 N#CC(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
155513751 169904 None 0 Human Binding pKi = 7.4 7.4 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169904 None 0 Human Binding pKi = 7.4 7.4 7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
22335694 171661 None 0 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 171661 None 0 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10571296 35488 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 371 6 1 4 4.0 Cn1cccc1C(C#N)CCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL143840 35488 None 0 Human Binding pKi = 6.4 6.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 371 6 1 4 4.0 Cn1cccc1C(C#N)CCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
22335694 171661 None 0 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 171661 None 0 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9804868 33846 None 1 Human Binding pKi = 7.4 7.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 472 5 1 4 6.0 N#CC1(CCCN2CCC(O)(c3ccc(F)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL142318 33846 None 1 Human Binding pKi = 7.4 7.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 472 5 1 4 6.0 N#CC1(CCCN2CCC(O)(c3ccc(F)cc3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
9956380 168352 None 0 Human Binding pKi = 7.4 7.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 470 5 1 3 6.0 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CCc2ccccc21 10.1021/jm990316l
CHEMBL433746 168352 None 0 Human Binding pKi = 7.4 7.4 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 470 5 1 3 6.0 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2CCc2ccccc21 10.1021/jm990316l
10786180 35472 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 382 6 1 3 4.9 CC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL143825 35472 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 382 6 1 3 4.9 CC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
10573219 35596 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 402 6 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm990316l
CHEMBL143942 35596 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 402 6 1 3 5.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm990316l
22335665 173571 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 173571 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
12093163 174506 None 0 Human Binding pKi = 6.3 6.3 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 174506 None 0 Human Binding pKi = 6.3 6.3 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
22335665 173571 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 173571 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10695227 35333 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 9 1 6 4.7 COc1cc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc(OC)c1OC 10.1021/jm990316l
CHEMBL143690 35333 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 9 1 6 4.7 COc1cc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc(OC)c1OC 10.1021/jm990316l
10195332 82599 None 0 Human Binding pKi = 8.3 8.3 - 1
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 461 9 4 6 3.4 CC(=O)Nc1ccc(O)cc1OC[C@@](C)(O)CNC1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm300682j
CHEMBL2178570 82599 None 0 Human Binding pKi = 8.3 8.3 - 1
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 461 9 4 6 3.4 CC(=O)Nc1ccc(O)cc1OC[C@@](C)(O)CNC1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm300682j
54671008 94979 None 64 Human Binding pKi = 8.3 8.3 - 1
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 444 6 3 9 0.9 Cc1nnc(C(=O)NC(C)(C)c2nc(C(=O)NCc3ccc(F)cc3)c(O)c(=O)n2C)o1 10.1021/jm300682j
CHEMBL254316 94979 None 64 Human Binding pKi = 8.3 8.3 - 1
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 444 6 3 9 0.9 Cc1nnc(C(=O)NC(C)(C)c2nc(C(=O)NCc3ccc(F)cc3)c(O)c(=O)n2C)o1 10.1021/jm300682j
155521447 170687 None 0 Human Binding pKi = 8.3 8.3 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170687 None 0 Human Binding pKi = 8.3 8.3 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
87496446 170881 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 542 7 2 6 4.6 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(=O)CO)CC2)c(Cl)cc1Cl nan
CHEMBL4452884 170881 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 542 7 2 6 4.6 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(=O)CO)CC2)c(Cl)cc1Cl nan
155521447 170687 None 0 Human Binding pKi = 8.3 8.3 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170687 None 0 Human Binding pKi = 8.3 8.3 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
155514261 169939 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169939 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
155514261 169939 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169939 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
12093163 174506 None 0 Human Binding pKi = 6.3 6.3 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 174506 None 0 Human Binding pKi = 6.3 6.3 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
15985914 84008 None 0 Human Binding pKi = 6.3 6.3 -8 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 84008 None 0 Human Binding pKi = 6.3 6.3 -8 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71450657 84022 None 0 Human Binding pKi = 6.3 6.3 -19 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207094 84022 None 0 Human Binding pKi = 6.3 6.3 -19 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
10789482 33693 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 444 9 1 3 5.9 N#CC(CCCCl)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL142191 33693 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 444 9 1 3 5.9 N#CC(CCCCl)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
10549688 165463 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 413 7 1 5 4.6 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc([N+](=O)[O-])c1 10.1021/jm990316l
CHEMBL423734 165463 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 413 7 1 5 4.6 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc([N+](=O)[O-])c1 10.1021/jm990316l
9889700 118652 None 11 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL34166 118652 None 11 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 444 7 1 3 5.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
9967465 172190 None 8 Human Binding pKi = 6.3 6.3 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 172190 None 8 Human Binding pKi = 6.3 6.3 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10764931 119332 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 426 7 1 5 4.0 COC(=O)C(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL343680 119332 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 426 7 1 5 4.0 COC(=O)C(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
10667913 33663 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 386 6 1 3 4.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm990316l
CHEMBL142161 33663 None 0 Human Binding pKi = 6.3 6.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 386 6 1 3 4.9 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm990316l
2868511 42644 None 8 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 337 4 1 4 3.5 COc1ccc(C2C(C(C)=O)=C(O)C(=O)N2c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL1500746 42644 None 8 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 337 4 1 4 3.5 COc1ccc(C2C(C(C)=O)=C(O)C(=O)N2c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.8b00605
10499297 34743 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 368 6 1 3 4.7 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL143059 34743 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 368 6 1 3 4.7 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
9870787 34872 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 504 5 1 4 5.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C[S+]([O-])c2ccccc21 10.1021/jm990316l
CHEMBL143173 34872 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 504 5 1 4 5.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C[S+]([O-])c2ccccc21 10.1021/jm990316l
9857981 170890 None 8 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170890 None 8 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9945265 171286 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 171286 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
2868511 42644 None 8 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 337 4 1 4 3.5 COc1ccc(C2C(C(C)=O)=C(O)C(=O)N2c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL1500746 42644 None 8 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 337 4 1 4 3.5 COc1ccc(C2C(C(C)=O)=C(O)C(=O)N2c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.8b00605
9967465 172190 None 8 Human Binding pKi = 6.3 6.3 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 172190 None 8 Human Binding pKi = 6.3 6.3 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9857981 170890 None 8 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170890 None 8 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9945265 171286 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 171286 None 0 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
9869274 119377 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C=Cc2ccccc21 10.1021/jm990316l
CHEMBL344073 119377 None 0 Human Binding pKi = 7.3 7.3 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C=Cc2ccccc21 10.1021/jm990316l
9924108 171876 None 0 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171876 None 0 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
9924108 171876 None 0 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171876 None 0 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
10737864 121637 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 369 6 1 4 4.1 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccn1 10.1021/jm990316l
CHEMBL358596 121637 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 369 6 1 4 4.1 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccn1 10.1021/jm990316l
11801020 12252 None 0 Human Binding pKi = 8.2 8.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 434 7 1 1 6.4 C[N+]1(CCCC(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL1184558 12252 None 0 Human Binding pKi = 8.2 8.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 434 7 1 1 6.4 C[N+]1(CCCC(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL356099 12252 None 0 Human Binding pKi = 8.2 8.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 434 7 1 1 6.4 C[N+]1(CCCC(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
24863549 170511 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 526 6 1 5 5.6 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(C)=O)CC2)c(Cl)cc1Cl nan
CHEMBL4448154 170511 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 526 6 1 5 5.6 COc1cc(N2CCC(C(Cn3nc(C(F)(F)F)c(Cl)c3C)NC(C)=O)CC2)c(Cl)cc1Cl nan
10768343 118806 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 522 5 1 4 6.9 N#CC1(CCCN2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
CHEMBL341769 118806 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 522 5 1 4 6.9 N#CC1(CCCN2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)c2ccccc2CSc2ccccc21 10.1021/jm990316l
155526680 171232 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 171232 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
155526680 171232 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 171232 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
3794409 170859 None 5 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170859 None 5 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
3794409 170859 None 5 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170859 None 5 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
9870787 34872 None 0 Human Binding pKi = 7.2 7.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 504 5 1 4 5.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C[S+]([O-])c2ccccc21 10.1021/jm990316l
CHEMBL143173 34872 None 0 Human Binding pKi = 7.2 7.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 504 5 1 4 5.5 N#CC1(CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc2C[S+]([O-])c2ccccc21 10.1021/jm990316l
10813846 31435 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 460 7 1 3 6.4 N#CC(CCCN1CCC(O)(c2ccc3ccccc3c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL140270 31435 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 460 7 1 3 6.4 N#CC(CCCN1CCC(O)(c2ccc3ccccc3c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
3497 1181 None 25 Human Binding pKi = 7.1 7.1 2 3
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1021/jm300682j
5311123 1181 None 25 Human Binding pKi = 7.1 7.1 2 3
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1021/jm300682j
CHEMBL1628706 1181 None 25 Human Binding pKi = 7.1 7.1 2 3
Binding affinity to CCR1Binding affinity to CCR1
ChEMBL 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 10.1021/jm300682j
10766998 34032 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 476 7 1 4 5.5 COc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1Br 10.1021/jm990316l
CHEMBL142468 34032 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 476 7 1 4 5.5 COc1ccc(C(C#N)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)cc1Br 10.1021/jm990316l
10693630 78876 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 424 8 1 3 5.3 N#CC(CCCN1CCC(CO)(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL2112830 78876 None 0 Human Binding pKi = 5.1 5.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 424 8 1 3 5.3 N#CC(CCCN1CCC(CO)(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
155548977 173899 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 375 4 1 3 5.0 Cc1ccc(N2C(=O)C(O)=C(C(=O)c3ccccc3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4538013 173899 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 375 4 1 3 5.0 Cc1ccc(N2C(=O)C(O)=C(C(=O)c3ccccc3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155548977 173899 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 375 4 1 3 5.0 Cc1ccc(N2C(=O)C(O)=C(C(=O)c3ccccc3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4538013 173899 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 375 4 1 3 5.0 Cc1ccc(N2C(=O)C(O)=C(C(=O)c3ccccc3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
10575889 33697 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 8 1 3 6.3 N#CC(CCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL142199 33697 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 458 8 1 3 6.3 N#CC(CCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
10643770 34408 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1O 10.1021/jm990316l
CHEMBL142798 34408 None 0 Human Binding pKi = 6.1 6.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1O 10.1021/jm990316l
71463165 84014 None 0 Human Binding pKi = 5.1 5.1 -6 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207086 84014 None 0 Human Binding pKi = 5.1 5.1 -6 2
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
71456007 84020 None 0 Human Binding pKi = 5.1 5.1 -5 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207092 84020 None 0 Human Binding pKi = 5.1 5.1 -5 3
Binding affinity to CCR1 by 35S-gamma-GTP membrane assayBinding affinity to CCR1 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
10722083 72603 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 459 7 1 2 6.1 C[N+]1(CCCC(C#N)(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL141127 72603 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 459 7 1 2 6.1 C[N+]1(CCCC(C#N)(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL199252 72603 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 459 7 1 2 6.1 C[N+]1(CCCC(C#N)(c2ccccc2)c2ccccc2)CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
3796276 170953 None 5 Human Binding pKi = 7.1 7.1 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170953 None 5 Human Binding pKi = 7.1 7.1 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
3796276 170953 None 5 Human Binding pKi = 7.1 7.1 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170953 None 5 Human Binding pKi = 7.1 7.1 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR1 expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
9959839 34358 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 574 10 4 4 5.4 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)NC1CCNCC1 10.1021/jm990316l
CHEMBL142752 34358 None 0 Human Binding pKi = 8.1 8.1 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 574 10 4 4 5.4 O=C(NCC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1)NC1CCNCC1 10.1021/jm990316l
10525695 121562 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 411 7 1 4 4.7 N#CC(CCCN1CCC(O)(c2ccccn2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL358283 121562 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 411 7 1 4 4.7 N#CC(CCCN1CCC(O)(c2ccccn2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
11798220 33778 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 460 8 1 4 6.5 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Oc2ccccc2)c1 10.1021/jm990316l
CHEMBL142263 33778 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 460 8 1 4 6.5 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cccc(Oc2ccccc2)c1 10.1021/jm990316l
10789018 35185 None 0 Human Binding pKi = 7.0 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 435 7 1 4 5.1 N#Cc1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
CHEMBL143499 35185 None 0 Human Binding pKi = 7.0 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 435 7 1 4 5.1 N#Cc1ccc(C2(O)CCN(CCCC(C#N)(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm990316l
10548809 119235 None 0 Human Binding pKi = 7.0 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 396 7 1 3 5.3 CCC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
CHEMBL343028 119235 None 0 Human Binding pKi = 7.0 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 396 7 1 3 5.3 CCC(C#N)(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/jm990316l
44199443 170642 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 378 6 2 3 4.0 CCC(NC(=O)C1CCCC1)C(O)C1CCN(c2ccc(Cl)cc2)CC1 nan
CHEMBL4449875 170642 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assayDisplacement of human [125I]-MIP-1alpha from CCR1 in human THP-1 cells incubated for 30 mins by radioligand binding assay
ChEMBL 378 6 2 3 4.0 CCC(NC(=O)C1CCCC1)C(O)C1CCN(c2ccc(Cl)cc2)CC1 nan
10810107 36927 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(O)cc1 10.1021/jm990316l
CHEMBL145106 36927 None 0 Human Binding pKi = 6.0 6.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 384 6 2 4 4.4 N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(O)cc1 10.1021/jm990316l
10572669 119505 None 0 Human Binding pKi = 7.0 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 393 6 1 4 4.6 N#Cc1ccccc1C(C#N)CCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
CHEMBL344989 119505 None 0 Human Binding pKi = 7.0 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 393 6 1 4 4.6 N#Cc1ccccc1C(C#N)CCCN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1021/jm990316l
10576419 34207 None 0 Human Binding pKi = 7 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 472 9 1 3 6.7 N#CC(CCCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
CHEMBL142620 34207 None 0 Human Binding pKi = 7 7.0 - 1
Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cellsInhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells
ChEMBL 472 9 1 3 6.7 N#CC(CCCCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm990316l
44537841 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.
Guide to Pharmacology 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 25101488
57889181 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.
Guide to Pharmacology 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 25101488
9497 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.
Guide to Pharmacology 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 25101488
CHEMBL2398716 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.
Guide to Pharmacology 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 25101488
CHEMBL3334824 675 None 16 Human Binding pIC50 = 9 9.0 - 1
Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.Displacement of [<sup>125</sup>I]MIP-1&alpha; from CCR1 in human THP-1 cells.
Guide to Pharmacology 438 6 3 4 3.1 O=C(CC(O)(C)C)N[C@@H](C(=O)N1CC[C@](C(C1)(C)C)(O)c1ccc(cc1)Cl)C(C)C 25101488
3497 1181 None 25 Human Binding pKd = 8 8.0 2 3
UnclassifiedUnclassified
Guide to Pharmacology 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 12909630
5311123 1181 None 25 Human Binding pKd = 8 8.0 2 3
UnclassifiedUnclassified
Guide to Pharmacology 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 12909630
CHEMBL1628706 1181 None 25 Human Binding pKd = 8 8.0 2 3
UnclassifiedUnclassified
Guide to Pharmacology 482 11 4 6 2.5 O[C@H]([C@@H](NC(=O)c1cnc2c(n1)cccc2)Cc1cccc(c1)F)C[C@H](C(=O)N)CCC(O)(C)C 12909630
54671008 94979 None 64 Human Binding pKi = 8.1 8.1 - 1
Binding affinity to CCR1Binding affinity to CCR1
Drug Central 444 6 3 9 0.9 Cc1nnc(C(=O)NC(C)(C)c2nc(C(=O)NCc3ccc(F)cc3)c(O)c(=O)n2C)o1 None
CHEMBL254316 94979 None 64 Human Binding pKi = 8.1 8.1 - 1
Binding affinity to CCR1Binding affinity to CCR1
Drug Central 444 6 3 9 0.9 Cc1nnc(C(=O)NC(C)(C)c2nc(C(=O)NCc3ccc(F)cc3)c(O)c(=O)n2C)o1 None
753 829 None 0 Human Binding pKi = 7.4 7.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12381680
757 862 None 0 Human Binding pKi = 7.5 7.5 -112 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12381680
757 862 None 0 Human Binding pKi = 7.5 7.5 -112 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8530354
758 865 None 0 Human Binding pKi = 7.5 7.5 -89 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8530354
758 865 None 0 Human Binding pKi = 7.5 7.5 -89 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9624164
759 866 None 0 Human Binding pKi = 8.1 8.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11994538
759 866 None 0 Human Binding pKi = 8.1 8.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12381680
512282 758 None 42 Human Binding pKi = 8.6 8.6 147 2
UnclassifiedUnclassified
Guide to Pharmacology 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10748002
767 758 None 42 Human Binding pKi = 8.6 8.6 147 2
UnclassifiedUnclassified
Guide to Pharmacology 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10748002
CHEMBL232656 758 None 42 Human Binding pKi = 8.6 8.6 147 2
UnclassifiedUnclassified
Guide to Pharmacology 434 6 2 4 3.1 NC(=O)Nc1cc(Cl)ccc1OCC(=O)N1CCN(C[C@H]1C)Cc1ccc(cc1)F 10748002
755 848 None 0 Human Binding pKi = 8.9 8.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12381680
756 859 None 0 Human Binding pKi = 9 9.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11170631
756 859 None 0 Human Binding pKi = 9 9.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12381680
756 859 None 0 Human Binding pKi = 9 9.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8530354
756 859 None 0 Human Binding pKi = 9 9.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9624164
760 1655 None 0 Human Binding pKi None 7.1 7.1 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11170631
752 710 None 0 Human Binding pKi None 8.8 8.8 12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11170631