Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
71461073 84167 1 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
71461074 84167 1 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181443 84167 1 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2221034 84167 1 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
127032486 138571 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 744 16 3 6 6.7 CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3786631 138571 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 744 16 3 6 6.7 CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127030694 138685 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3786670 138685 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787750 138685 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127031313 138616 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 822 17 3 8 6.1 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(S(C)(=O)=O)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787121 138616 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 822 17 3 8 6.1 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(S(C)(=O)=O)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
71455657 84117 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 474 5 0 0 6.6 CC1(C)[C@H]2CC[C@@H](C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181446 84117 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 474 5 0 0 6.6 CC1(C)[C@H]2CC[C@@H](C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220411 84117 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 474 5 0 0 6.6 CC1(C)[C@H]2CC[C@@H](C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 10.1021/jm301240t
71450270 84121 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 360 5 0 0 6.2 Cc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
CHEMBL2181464 84121 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 360 5 0 0 6.2 Cc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
CHEMBL2220445 84121 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 360 5 0 0 6.2 Cc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
71459297 84126 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 364 5 0 0 6.1 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4F)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181451 84126 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 364 5 0 0 6.1 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4F)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220493 84126 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 364 5 0 0 6.1 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4F)cc3)[C@@H]1C2 10.1021/jm301240t
71455653 84129 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 376 6 0 1 5.9 COc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
CHEMBL2181441 84129 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 376 6 0 1 5.9 COc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
CHEMBL2220506 84129 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 376 6 0 1 5.9 COc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
127032747 138467 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 744 16 3 6 6.7 CC(C)(C)OC(=O)NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3785515 138467 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 744 16 3 6 6.7 CC(C)(C)OC(=O)NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
71457436 84123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@@H]2C=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)C[C@H]1C2 10.1021/jm301240t
CHEMBL2181448 84123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@@H]2C=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)C[C@H]1C2 10.1021/jm301240t
CHEMBL2220478 84123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@@H]2C=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)C[C@H]1C2 10.1021/jm301240t
71452094 84127 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 380 5 0 0 6.6 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181452 84127 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 380 5 0 0 6.6 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220494 84127 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 380 5 0 0 6.6 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
71453926 84132 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4c(Cl)cccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181460 84132 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4c(Cl)cccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220526 84132 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4c(Cl)cccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
127030984 138641 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 584 12 4 5 4.8 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787404 138641 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 584 12 4 5 4.8 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127032169 138682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 484 11 4 4 3.3 N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787326 138682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 484 11 4 4 3.3 N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787718 138682 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 484 11 4 4 3.3 N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127032453 138548 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 804 18 3 8 6.7 COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1OC 10.1021/acs.jmedchem.5b01965
CHEMBL3786459 138548 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 804 18 3 8 6.7 COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1OC 10.1021/acs.jmedchem.5b01965
71462816 84161 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cc(Cl)ccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181459 84161 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cc(Cl)ccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220967 84161 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cc(Cl)ccc4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
127030991 138555 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 762 16 3 6 6.9 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(F)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3786522 138555 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 762 16 3 6 6.9 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(F)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
71457439 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL2181467 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787171 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127031312 138566 2 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 774 17 3 7 6.7 COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/acs.jmedchem.5b01965
CHEMBL3786577 138566 2 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 774 17 3 7 6.7 COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/acs.jmedchem.5b01965
71457439 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/jm301240t
CHEMBL2181467 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/jm301240t
CHEMBL3787171 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/jm301240t
71450266 84125 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@H]1C2 10.1021/jm301240t
CHEMBL2181450 84125 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@H]1C2 10.1021/jm301240t
CHEMBL2220492 84125 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 472 5 0 0 6.5 CC1(C)[C@@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@H]1C2 10.1021/jm301240t
71455659 84131 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cccc(Cl)c4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181458 84131 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cccc(Cl)c4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220525 84131 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cccc(Cl)c4Cl)cc3)[C@@H]1C2 10.1021/jm301240t
71457439 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL2181467 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787171 82613 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
71459295 84115 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 424 5 0 0 6.7 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Br)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181442 84115 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 424 5 0 0 6.7 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Br)cc3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220409 84115 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 424 5 0 0 6.7 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Br)cc3)[C@@H]1C2 10.1021/jm301240t
71459301 84120 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)c(Cl)c3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2181463 84120 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)c(Cl)c3)[C@@H]1C2 10.1021/jm301240t
CHEMBL2220444 84120 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 414 5 0 0 7.2 CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)c(Cl)c3)[C@@H]1C2 10.1021/jm301240t
71450272 84122 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 374 5 0 0 6.5 Cc1cccc(C)c1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
CHEMBL2181465 84122 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 374 5 0 0 6.5 Cc1cccc(C)c1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
CHEMBL2220446 84122 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at CXCR3 expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 374 5 0 0 6.5 Cc1cccc(C)c1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 10.1021/jm301240t
127032454 138471 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 730 16 3 5 7.1 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3785564 138471 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 730 16 3 5 7.1 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127032455 138657 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 716 15 3 5 6.7 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787609 138657 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 716 15 3 5 6.7 CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
127031901 138683 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787077 138683 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
CHEMBL3787719 138683 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assayPositive allosteric modulation of human CXCR3 expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 644 15 3 5 5.2 N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.5b01965
11569938 57913 0 None 5 3 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 521 7 1 5 4.8 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681882 57913 0 None 5 3 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 521 7 1 5 4.8 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
44592137 178599 1 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 503 7 1 5 4.7 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL472288 178599 1 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 503 7 1 5 4.7 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
45101529 5594 0 None 1 4 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to IP10 in bufferAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to IP10 in buffer
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077831 5594 0 None 1 4 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to IP10 in bufferAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to IP10 in buffer
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
44592137 178599 1 None -1 3 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse CXCR3Antagonist activity at mouse CXCR3
ChEMBL 503 7 1 5 4.7 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL472288 178599 1 None -1 3 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse CXCR3Antagonist activity at mouse CXCR3
ChEMBL 503 7 1 5 4.7 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
45101529 5594 0 None 1 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to MIG in bufferAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to MIG in buffer
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077831 5594 0 None 1 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to MIG in bufferAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to MIG in buffer
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
45101529 5594 0 None 1 4 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in RPMI bufferAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in RPMI buffer
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077831 5594 0 None 1 4 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in RPMI bufferAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in RPMI buffer
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
11569938 57913 0 None -5 3 Mouse 9.0 pIC50 = 9.0 Functional
Antagonist activity at mouse CXCR3Antagonist activity at mouse CXCR3
ChEMBL 521 7 1 5 4.8 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681882 57913 0 None -5 3 Mouse 9.0 pIC50 = 9.0 Functional
Antagonist activity at mouse CXCR3Antagonist activity at mouse CXCR3
ChEMBL 521 7 1 5 4.8 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
44592137 178599 1 None -3 3 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat CXCR3Antagonist activity at rat CXCR3
ChEMBL 503 7 1 5 4.7 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL472288 178599 1 None -3 3 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat CXCR3Antagonist activity at rat CXCR3
ChEMBL 503 7 1 5 4.7 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
89725838 145351 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 573 5 1 9 3.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
CHEMBL3917642 145351 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 573 5 1 9 3.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
71679146 152875 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 526 4 1 8 4.2 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00676
CHEMBL3978935 152875 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 526 4 1 8 4.2 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00676
11569938 57913 0 None -7 3 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat CXCR3Antagonist activity at rat CXCR3
ChEMBL 521 7 1 5 4.8 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681882 57913 0 None -7 3 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat CXCR3Antagonist activity at rat CXCR3
ChEMBL 521 7 1 5 4.8 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
71679146 152875 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 526 4 1 8 4.2 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
CHEMBL3978935 152875 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 526 4 1 8 4.2 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
168278609 190401 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 474 5 1 6 3.7 O=C(Nc1ccccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.2c00675
CHEMBL5186472 190401 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 474 5 1 6 3.7 O=C(Nc1ccccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.2c00675
117739261 146272 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 509 4 1 7 4.3 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 10.1021/acs.jmedchem.2c00676
CHEMBL3924716 146272 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 509 4 1 7 4.3 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 10.1021/acs.jmedchem.2c00676
12207 272 5 None 7 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
87056189 272 5 None 7 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
CHEMBL5202301 272 5 None 7 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
89725785 142570 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 486 5 1 8 3.7 CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 10.1021/acs.jmedchem.2c00675
CHEMBL3895485 142570 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 486 5 1 8 3.7 CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 10.1021/acs.jmedchem.2c00675
46883304 5587 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 639 10 0 7 6.3 CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3C(C)C)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077824 5587 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 639 10 0 7 6.3 CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3C(C)C)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
44453468 154547 0 None 77 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 9 1 6 6.4 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CCCN(C(=O)c1cccc2cccnc12)C1CC1 10.1016/j.bmcl.2008.02.049
CHEMBL401868 154547 0 None 77 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 9 1 6 6.4 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CCCN(C(=O)c1cccc2cccnc12)C1CC1 10.1016/j.bmcl.2008.02.049
56670465 63893 0 None -1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 400 2 2 2 3.7 CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1808996 63893 0 None -1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 400 2 2 2 3.7 CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
168287429 190887 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 582 5 1 10 3.1 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(S(C)(=O)=O)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL5193530 190887 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 582 5 1 10 3.1 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(S(C)(=O)=O)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
56670465 63893 0 None 1 2 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 400 2 2 2 3.7 CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1808996 63893 0 None 1 2 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 400 2 2 2 3.7 CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
56677273 63921 0 None 1 2 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 432 2 2 3 4.3 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccs2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809025 63921 0 None 1 2 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 432 2 2 3 4.3 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccs2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
44453232 94956 0 None 12 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 502 10 1 5 5.1 CCc1cccc2c1n(CCCN(C)C(=O)Cc1ccccc1)c(=N)n2CC(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.02.049
CHEMBL256891 94956 0 None 12 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 502 10 1 5 5.1 CCc1cccc2c1n(CCCN(C)C(=O)Cc1ccccc1)c(=N)n2CC(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.02.049
45482807 196482 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assay
ChEMBL 442 4 2 2 4.8 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(C)cc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL574831 196482 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assay
ChEMBL 442 4 2 2 4.8 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(C)cc2)C1 10.1016/j.bmcl.2009.09.002
45486493 196746 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 601 9 0 7 5.3 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccn2c1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL577108 196746 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 601 9 0 7 5.3 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccn2c1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
11296495 72385 15 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of CXCL11-induced CXCR3 mediated T-cell migrationInhibition of CXCL11-induced CXCR3 mediated T-cell migration
ChEMBL 615 8 3 4 6.1 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL199839 72385 15 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of CXCL11-induced CXCR3 mediated T-cell migrationInhibition of CXCL11-induced CXCR3 mediated T-cell migration
ChEMBL 615 8 3 4 6.1 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
44581090 187338 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 441 4 1 4 3.4 O=C1CCC(c2cccnc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL496771 187338 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 441 4 1 4 3.4 O=C1CCC(c2cccnc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
44580799 187522 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 456 4 2 4 3.7 O=C1CCC(c2cccc(O)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL498199 187522 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 456 4 2 4 3.7 O=C1CCC(c2cccc(O)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
44580878 187573 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 500 6 0 4 5.1 CSCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O 10.1016/j.bmcl.2008.07.115
CHEMBL498555 187573 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 500 6 0 4 5.1 CSCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O 10.1016/j.bmcl.2008.07.115
44570312 177036 0 None -7 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 460 4 0 6 2.7 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
CHEMBL464083 177036 0 None -7 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 460 4 0 6 2.7 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
56670455 63927 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 430 3 2 3 3.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccco2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809034 63927 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 430 3 2 3 3.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccco2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
57400629 69625 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serumAntagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serum
ChEMBL 624 9 0 7 5.2 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.10.120
CHEMBL1939557 69625 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serumAntagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serum
ChEMBL 624 9 0 7 5.2 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.10.120
168283702 190172 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 522 4 0 9 3.9 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00675
CHEMBL5183171 190172 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 522 4 0 9 3.9 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00675
168287733 191207 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 517 5 0 9 3.7 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5198351 191207 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 517 5 0 9 3.7 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
89726154 151446 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 472 4 1 8 3.5 Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 10.1021/acs.jmedchem.2c00675
CHEMBL3966706 151446 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 472 4 1 8 3.5 Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 10.1021/acs.jmedchem.2c00675
57393685 69626 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serumAntagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serum
ChEMBL 624 9 0 7 5.2 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.10.120
CHEMBL1939558 69626 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serumAntagonist activity at CXCR3 assessed as inhibition of ITAC-mediated cell migration in presence of 100% human serum
ChEMBL 624 9 0 7 5.2 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.10.120
46891329 6752 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 425 7 1 5 3.2 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)O)c(F)c2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083956 6752 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 425 7 1 5 3.2 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)O)c(F)c2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
56673942 63923 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 432 2 2 2 4.1 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809028 63923 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 432 2 2 2 4.1 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
56673940 63920 0 None 1 2 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 432 2 2 3 4.3 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccsc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809024 63920 0 None 1 2 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 432 2 2 3 4.3 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccsc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
53322459 57867 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 489 5 1 5 4.5 CNC(=O)c1cnc(N2CCN(C3CCN(C(C)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681832 57867 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 489 5 1 5 4.5 CNC(=O)c1cnc(N2CCN(C3CCN(C(C)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
24739387 187574 0 None 9 4 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL498556 187574 0 None 9 4 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
89726171 143096 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 489 4 0 8 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3n2C)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
CHEMBL3899775 143096 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 489 4 0 8 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3n2C)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
56673938 63903 0 None -1 2 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 455 2 2 3 3.4 CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809006 63903 0 None -1 2 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 455 2 2 3 3.4 CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 10.1016/j.bmcl.2011.06.070
46891327 6750 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 434 7 1 4 4.0 O=C(O)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2010.04.113
CHEMBL1083954 6750 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 434 7 1 4 4.0 O=C(O)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2010.04.113
89726281 148236 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 571 5 1 11 3.2 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-n5cncn5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3940550 148236 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 571 5 1 11 3.2 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-n5cncn5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
16040696 94356 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL253431 94356 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.032
16040696 94356 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CXCR3 assessed as ITAC-mediated migration of human PBMC in presence of 100% human plasmaAntagonist activity at CXCR3 assessed as ITAC-mediated migration of human PBMC in presence of 100% human plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2007.11.060
CHEMBL253431 94356 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CXCR3 assessed as ITAC-mediated migration of human PBMC in presence of 100% human plasmaAntagonist activity at CXCR3 assessed as ITAC-mediated migration of human PBMC in presence of 100% human plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2007.11.060
16040696 94356 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL253431 94356 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
46891223 7194 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 465 10 1 5 3.6 COc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NCC3CC3)cc2)Cc2cccnc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1085998 7194 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 465 10 1 5 3.6 COc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NCC3CC3)cc2)Cc2cccnc2)cc1 10.1016/j.bmcl.2010.04.113
90480414 190075 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 495 5 0 9 3.2 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5181702 190075 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 495 5 0 9 3.2 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
168287236 191130 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 550 6 0 10 3.4 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc(C(F)(F)F)n3)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5197175 191130 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 550 6 0 10 3.4 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc(C(F)(F)F)n3)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
56660099 63895 0 None -3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 430 4 3 3 3.1 CN(CCO)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1808998 63895 0 None -3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 430 4 3 3 3.1 CN(CCO)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
56670449 63911 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 3 3 3.2 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1809014 63911 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 3 3 3.2 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 10.1016/j.bmcl.2011.06.070
56660101 63905 0 None 1 3 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 2 3 3.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809008 63905 0 None 1 3 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 2 3 3.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 10.1016/j.bmcl.2011.06.070
45486525 196876 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 615 10 0 7 5.6 CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 10.1016/j.bmcl.2009.07.021
CHEMBL578189 196876 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 615 10 0 7 5.6 CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 10.1016/j.bmcl.2009.07.021
44593651 187154 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 476 4 1 3 4.3 O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL495531 187154 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 476 4 1 3 4.3 O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
15604606 140042 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 581 8 3 4 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL381227 140042 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 581 8 3 4 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
89725838 145351 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 573 5 1 9 3.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
CHEMBL3917642 145351 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 573 5 1 9 3.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
117740233 153127 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 588 5 1 9 4.5 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3981151 153127 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 588 5 1 9 4.5 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
44570312 177036 0 None 7 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 460 4 0 6 2.7 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
CHEMBL464083 177036 0 None 7 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 460 4 0 6 2.7 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
15604608 72271 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 533 7 3 4 4.8 CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccccc3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL199408 72271 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 533 7 3 4 4.8 CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccccc3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
53325132 57891 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 475 5 1 5 3.9 CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)C[C@@H]3C)CC2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681859 57891 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 475 5 1 5 3.9 CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)C[C@@H]3C)CC2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
27307547 177031 1 None -5 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 445 4 0 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL464081 177031 1 None -5 2 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 445 4 0 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
89726625 151939 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 536 4 1 8 3.9 C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
CHEMBL3971056 151939 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 536 4 1 8 3.9 C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
44581087 187508 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 430 4 1 3 4.6 O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL498012 187508 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 430 4 1 3 4.6 O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
44580797 187521 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 581 6 2 6 2.9 CN(C(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1)N1CCNCC1 10.1016/j.bmcl.2008.07.115
CHEMBL498198 187521 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 581 6 2 6 2.9 CN(C(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1)N1CCNCC1 10.1016/j.bmcl.2008.07.115
44581162 188948 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 541 8 3 5 3.1 O=C1CCC(c2cccc(C(=O)NCCCO)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL514259 188948 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 541 8 3 5 3.1 O=C1CCC(c2cccc(C(=O)NCCCO)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
44581109 192487 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 458 4 1 3 4.2 O=C1CCC(c2ccc(F)cc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL522551 192487 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 458 4 1 3 4.2 O=C1CCC(c2ccc(F)cc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
45486560 196880 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL578197 196880 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 615 9 0 8 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
44253589 6399 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 473 7 1 5 4.6 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1cccc(Cl)c1 10.1016/j.bmcl.2010.04.113
CHEMBL1082649 6399 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 473 7 1 5 4.6 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1cccc(Cl)c1 10.1016/j.bmcl.2010.04.113
44253167 6556 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 538 9 1 3 6.3 O=C(NCc1cccc(Cl)c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083315 6556 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 538 9 1 3 6.3 O=C(NCc1cccc(Cl)c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
56673937 63897 0 None -2 3 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometryAntagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometry
ChEMBL 440 2 2 2 4.7 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809000 63897 0 None -2 3 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometryAntagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometry
ChEMBL 440 2 2 2 4.7 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 10.1016/j.bmcl.2011.06.070
46891272 6346 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 522 9 1 5 4.8 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NC3(c4ccccc4)CC3)cc2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1082388 6346 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 522 9 1 5 4.8 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NC3(c4ccccc4)CC3)cc2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
117740035 153319 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 475 4 1 7 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
CHEMBL3982804 153319 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 475 4 1 7 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
56660100 63898 0 None 2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 454 2 2 2 5.0 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809001 63898 0 None 2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 454 2 2 2 5.0 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 10.1016/j.bmcl.2011.06.070
168284279 190946 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 516 5 0 8 4.3 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 10.1021/acs.jmedchem.2c00675
CHEMBL5194504 190946 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 516 5 0 8 4.3 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 10.1021/acs.jmedchem.2c00675
15604689 72249 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 587 8 3 5 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccs2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL199321 72249 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 587 8 3 5 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccs2)CC1 10.1016/j.bmcl.2005.09.020
44406348 132304 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 616 8 2 5 6.5 CCOC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL370167 132304 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 616 8 2 5 6.5 CCOC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
46883309 6101 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 639 8 0 7 5.5 CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)=O)CC3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1081164 6101 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 639 8 0 7 5.5 CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)=O)CC3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
168284279 190946 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 516 5 0 8 4.3 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 10.1021/acs.jmedchem.2c00675
CHEMBL5194504 190946 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 516 5 0 8 4.3 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 10.1021/acs.jmedchem.2c00675
14479864 4583 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 440 4 1 3 4.0 O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL10309 4583 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 440 4 1 3 4.0 O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
117739191 150151 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 544 4 1 8 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CCN(C)C2 10.1021/acs.jmedchem.2c00676
CHEMBL3955848 150151 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 544 4 1 8 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CCN(C)C2 10.1021/acs.jmedchem.2c00676
90479878 189649 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 524 6 0 10 3.4 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC(C)C)nc3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00675
CHEMBL5175118 189649 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 524 6 0 10 3.4 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC(C)C)nc3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00675
168286976 190796 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 570 5 1 7 4.9 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)OC[C@@H]1c1ccccc1 10.1021/acs.jmedchem.2c00676
CHEMBL5192464 190796 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 570 5 1 7 4.9 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)OC[C@@H]1c1ccccc1 10.1021/acs.jmedchem.2c00676
56660100 63898 0 None -2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 454 2 2 2 5.0 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809001 63898 0 None -2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 454 2 2 2 5.0 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 10.1016/j.bmcl.2011.06.070
56667009 63924 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 446 2 2 2 4.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809029 63924 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 446 2 2 2 4.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
11964007 63896 0 None 1 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 412 2 2 2 3.9 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1808999 63896 0 None 1 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 412 2 2 2 3.9 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC1 10.1016/j.bmcl.2011.06.070
71680139 147163 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 500 5 1 8 4.3 CC(C)c1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 10.1021/acs.jmedchem.2c00675
CHEMBL3931920 147163 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 500 5 1 8 4.3 CC(C)c1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 10.1021/acs.jmedchem.2c00675
90480006 190214 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 494 5 0 9 3.1 CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5183818 190214 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 494 5 0 9 3.1 CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
44426723 85606 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 602 10 0 7 6.4 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL230664 85606 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 602 10 0 7 6.4 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
53323853 57909 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 519 6 1 7 3.1 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(C(=O)OC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681877 57909 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 519 6 1 7 3.1 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(C(=O)OC)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
24739387 187574 0 None 9 4 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL498556 187574 0 None 9 4 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
168296640 191876 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 575 8 0 11 3.0 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(OCCN(C)C)nc2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
CHEMBL5208823 191876 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 575 8 0 11 3.0 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(OCCN(C)C)nc2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
53325131 57889 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 587 7 1 5 4.9 O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(=O)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681857 57889 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 587 7 1 5 4.9 O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(=O)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
89726463 153570 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 542 4 2 8 3.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 10.1021/acs.jmedchem.2c00676
CHEMBL3985006 153570 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 542 4 2 8 3.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 10.1021/acs.jmedchem.2c00676
90480006 190214 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 494 5 0 9 3.1 CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5183818 190214 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 494 5 0 9 3.1 CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
89726174 146586 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 586 6 1 10 4.2 COc1cc2nc(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2cc1OC 10.1021/acs.jmedchem.2c00676
CHEMBL3927485 146586 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 586 6 1 10 4.2 COc1cc2nc(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2cc1OC 10.1021/acs.jmedchem.2c00676
44581136 192641 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 474 4 1 3 4.7 O=C1CCC(c2cccc(Cl)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
CHEMBL523748 192641 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 474 4 1 3 4.7 O=C1CCC(c2cccc(Cl)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 10.1016/j.bmcl.2008.07.115
44253591 6401 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 469 8 1 6 3.9 COc1cccc(CN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.113
CHEMBL1082660 6401 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 469 8 1 6 3.9 COc1cccc(CN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.113
168284829 191187 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 576 6 1 10 3.4 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5COC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL5198121 191187 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 576 6 1 10 3.4 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5COC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
45101529 5594 0 None 1 4 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077831 5594 0 None 1 4 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 688 11 0 8 5.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 10.1016/j.bmcl.2009.07.032
24957182 152979 37 None 63 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CXCR3 assessed as ITAC-mediated cell migrationAntagonist activity at CXCR3 assessed as ITAC-mediated cell migration
ChEMBL 603 10 0 8 5.8 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2007.11.060
CHEMBL397983 152979 37 None 63 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CXCR3 assessed as ITAC-mediated cell migrationAntagonist activity at CXCR3 assessed as ITAC-mediated cell migration
ChEMBL 603 10 0 8 5.8 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2007.11.060
89726091 146503 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 572 5 1 8 4.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 10.1021/acs.jmedchem.2c00676
CHEMBL3926820 146503 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 572 5 1 8 4.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 10.1021/acs.jmedchem.2c00676
168288302 190775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 528 4 1 6 4.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 10.1021/acs.jmedchem.2c00676
CHEMBL5192187 190775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 528 4 1 6 4.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 10.1021/acs.jmedchem.2c00676
24957182 152979 37 None 63 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of ITAC-induced CXCR3 mediated cell migrationInhibition of ITAC-induced CXCR3 mediated cell migration
ChEMBL 603 10 0 8 5.8 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2007.03.106
CHEMBL397983 152979 37 None 63 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of ITAC-induced CXCR3 mediated cell migrationInhibition of ITAC-induced CXCR3 mediated cell migration
ChEMBL 603 10 0 8 5.8 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2007.03.106
24739386 187195 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 440 5 0 2 4.9 O=CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL495752 187195 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 440 5 0 2 4.9 O=CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
89726765 148735 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 533 7 0 9 3.8 COCCn1c(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)nc2ccccc21 10.1021/acs.jmedchem.2c00676
CHEMBL3944489 148735 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 533 7 0 9 3.8 COCCn1c(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)nc2ccccc21 10.1021/acs.jmedchem.2c00676
44581134 187315 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 470 5 1 4 4.0 COc1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 10.1016/j.bmcl.2008.07.115
CHEMBL496570 187315 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 470 5 1 4 4.0 COc1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 10.1016/j.bmcl.2008.07.115
46891537 6337 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 475 7 1 5 4.2 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)c(F)c1)Cc1ccccc1F 10.1016/j.bmcl.2010.04.113
CHEMBL1082360 6337 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 475 7 1 5 4.2 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)c(F)c1)Cc1ccccc1F 10.1016/j.bmcl.2010.04.113
46891536 7095 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 454 8 1 7 2.8 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1085508 7095 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 454 8 1 7 2.8 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
44569942 176131 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 447 4 1 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL459950 176131 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 447 4 1 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(O)C2 10.1016/j.bmcl.2008.11.008
44570549 177798 0 None 15 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 459 4 0 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
CHEMBL465283 177798 0 None 15 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 459 4 0 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
44570385 182483 0 None 5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 463 4 0 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL479426 182483 0 None 5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 463 4 0 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
44570219 183322 0 None 3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 461 4 1 5 3.1 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
CHEMBL481197 183322 0 None 3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 461 4 1 5 3.1 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
44570272 177011 0 None -3 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 479 4 1 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
CHEMBL464064 177011 0 None -3 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 479 4 1 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
44580960 187579 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 426 4 1 2 4.5 O=C1NCCCC1(c1ccccc1)C1CCN(Cc2ccc(Br)cc2)CC1 10.1016/j.bmcl.2008.07.115
CHEMBL498620 187579 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 426 4 1 2 4.5 O=C1NCCCC1(c1ccccc1)C1CCN(Cc2ccc(Br)cc2)CC1 10.1016/j.bmcl.2008.07.115
44569941 175996 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 445 4 0 5 2.9 CC1(C)[C@@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL459742 175996 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 445 4 0 5 2.9 CC1(C)[C@@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
44570341 189279 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 455 4 0 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(Br)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL516872 189279 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 455 4 0 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(Br)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
44570273 177012 0 None -25 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 479 4 1 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
CHEMBL464065 177012 0 None -25 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 479 4 1 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
44570274 177160 0 None -39 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 521 4 0 6 3.6 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC24OCCO4)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
CHEMBL464244 177160 0 None -39 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 521 4 0 6 3.6 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC24OCCO4)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
44570629 183244 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 459 5 1 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)NC1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL480601 183244 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 459 5 1 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)NC1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
44570515 189347 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 427 4 0 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cc4ccccc4cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL517024 189347 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 427 4 0 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cc4ccccc4cn3)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
45101497 57882 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 619 7 1 5 6.8 C[C@H]1CN(c2ncc(C(=O)NCc3ccc(Cl)c(Cl)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
CHEMBL1681850 57882 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 619 7 1 5 6.8 C[C@H]1CN(c2ncc(C(=O)NCc3ccc(Cl)c(Cl)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
56660101 63905 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 2 3 3.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809008 63905 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 2 3 3.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 10.1016/j.bmcl.2011.06.070
56667007 63912 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 444 2 2 2 4.4 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809015 63912 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 444 2 2 2 4.4 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
56667009 63924 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 446 2 2 2 4.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809029 63924 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 446 2 2 2 4.5 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
46883310 5592 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 598 8 0 7 5.6 CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCOCC3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077829 5592 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 598 8 0 7 5.6 CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCOCC3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
168280397 190686 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 495 6 0 9 3.3 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5190681 190686 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 495 6 0 9 3.3 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
168288472 191123 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 502 4 0 9 3.4 Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5197065 191123 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 502 4 0 9 3.4 Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
89726091 146503 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 572 5 1 8 4.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 10.1021/acs.jmedchem.2c00676
CHEMBL3926820 146503 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 572 5 1 8 4.4 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 10.1021/acs.jmedchem.2c00676
46883297 5580 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 654 9 0 6 7.6 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077817 5580 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 654 9 0 6 7.6 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
53318510 57868 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 509 5 1 5 4.6 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4Cl)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681833 57868 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 509 5 1 5 4.6 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4Cl)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
45486526 195933 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 627 10 0 7 5.9 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL570665 195933 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 627 10 0 7 5.9 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
44581135 187316 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 550 6 2 6 3.3 COc1ccc(S(=O)(=O)O)cc1C1(C2CCN(Cc3ccc(Br)cc3)CC2)CCC(=O)NC1=O 10.1016/j.bmcl.2008.07.115
CHEMBL496571 187316 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 550 6 2 6 3.3 COc1ccc(S(=O)(=O)O)cc1C1(C2CCN(Cc3ccc(Br)cc3)CC2)CCC(=O)NC1=O 10.1016/j.bmcl.2008.07.115
56670456 63929 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 425 3 1 2 3.8 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Cc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809036 63929 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 425 3 1 2 3.8 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Cc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
15604607 132915 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 611 9 3 5 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(OC)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL370591 132915 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 611 9 3 5 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(OC)c2)CC1 10.1016/j.bmcl.2005.09.020
89726443 150340 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 488 5 2 9 2.7 C[C@@H]1CN(c2sc(CO)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
CHEMBL3957343 150340 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 488 5 2 9 2.7 C[C@@H]1CN(c2sc(CO)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
90480455 190679 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 510 6 0 10 3.0 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5190588 190679 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 510 6 0 10 3.0 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
56667005 63901 0 None -2 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 441 2 3 3 3.1 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809004 63901 0 None -2 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 441 2 3 3 3.1 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 10.1016/j.bmcl.2011.06.070
168271845 189956 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 475 5 1 7 3.1 O=C(Nc1ncccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.2c00675
CHEMBL5179925 189956 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 475 5 1 7 3.1 O=C(Nc1ncccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.2c00675
168273430 190091 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 518 5 0 10 3.1 COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5181928 190091 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 518 5 0 10 3.1 COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
53326388 57870 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 493 5 1 5 4.1 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681835 57870 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 493 5 1 5 4.1 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
45482789 197247 0 None 1 14 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assay
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 197247 0 None 1 14 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assay
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
45482789 197247 0 None 1 14 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
CHEMBL584554 197247 0 None 1 14 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
90480414 190075 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 495 5 0 9 3.2 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5181702 190075 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 495 5 0 9 3.2 COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
45486561 195976 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 645 10 0 9 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL570919 195976 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 645 10 0 9 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
45486522 196850 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 617 10 0 8 5.0 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL577973 196850 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 617 10 0 8 5.0 CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
45379650 196878 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 653 8 0 7 6.3 C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 10.1016/j.bmcl.2009.07.021
CHEMBL578192 196878 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 653 8 0 7 6.3 C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 10.1016/j.bmcl.2009.07.021
44580903 187256 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 466 5 0 3 5.0 O=C1CC1N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL496176 187256 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 466 5 0 3 5.0 O=C1CC1N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
46890724 7212 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 482 7 0 3 6.4 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2cccc(Cl)c2)cc1)Cc1ccccn1 10.1016/j.bmcl.2010.04.113
CHEMBL1086040 7212 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 482 7 0 3 6.4 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2cccc(Cl)c2)cc1)Cc1ccccn1 10.1016/j.bmcl.2010.04.113
56660098 63894 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 488 8 2 4 3.8 COCCN(CCOC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1808997 63894 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 488 8 2 4 3.8 COCCN(CCOC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2011.06.070
56673431 63602 0 None -63 3 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometryAntagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometry
ChEMBL 426 2 2 2 4.3 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1806523 63602 0 None -63 3 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometryAntagonist activity at CXCR3 in rat leukocytes assessed as inhibition of ITAC-induced cell migration by flow cytometry
ChEMBL 426 2 2 2 4.3 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
56670449 63911 0 None 1 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 3 3 3.2 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1809014 63911 0 None 1 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 3 3 3.2 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 10.1016/j.bmcl.2011.06.070
90479919 190780 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 480 4 0 9 2.9 Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5192208 190780 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 480 4 0 9 2.9 Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
44406319 73805 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 581 8 3 4 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL202289 73805 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 581 8 3 4 5.5 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
117740035 153319 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 475 4 1 7 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
CHEMBL3982804 153319 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 475 4 1 7 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 10.1021/acs.jmedchem.2c00676
46891078 6557 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 510 9 1 4 5.7 O=C(NCc1cccs1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083316 6557 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 510 9 1 4 5.7 O=C(NCc1cccs1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
46700871 7096 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 466 7 1 6 3.4 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccc2F)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1085509 7096 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 466 7 1 6 3.4 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccc2F)cc1 10.1016/j.bmcl.2010.04.113
45482814 196613 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assay
ChEMBL 430 4 2 2 4.6 CCN(CC)C(=O)[C@@H]1CC2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL575890 196613 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in L1.2 cells assessed as inhibition of I-TAC-induced Ca2+ mobilization by FLIPR assay
ChEMBL 430 4 2 2 4.6 CCN(CC)C(=O)[C@@H]1CC2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
53318512 57874 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 447 5 1 6 3.3 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4cccs4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681840 57874 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 447 5 1 6 3.3 CNC(=O)c1cnc(N2CCN(C3CCN(Cc4cccs4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
44253169 6738 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 468 9 1 3 4.9 O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083929 6738 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 468 9 1 3 4.9 O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
44569944 176132 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 461 4 1 5 3.1 CC1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C 10.1016/j.bmcl.2008.11.008
CHEMBL459951 176132 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 461 4 1 5 3.1 CC1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C 10.1016/j.bmcl.2008.11.008
44570029 178151 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 489 4 0 6 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C1(C2)OCCO1 10.1016/j.bmcl.2008.11.008
CHEMBL468468 178151 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 489 4 0 6 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C1(C2)OCCO1 10.1016/j.bmcl.2008.11.008
25265835 177154 0 None -6 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 479 4 1 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
CHEMBL464234 177154 0 None -6 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 479 4 1 5 3.3 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F 10.1016/j.bmcl.2008.11.008
44570220 183323 0 None -6 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 461 4 1 5 3.1 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
CHEMBL481198 183323 0 None -6 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse recombinant CXCR3 expressed in human U2OS cellsAntagonist activity at mouse recombinant CXCR3 expressed in human U2OS cells
ChEMBL 461 4 1 5 3.1 C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 10.1016/j.bmcl.2008.11.008
44570470 183246 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 462 4 0 4 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cc3F)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
CHEMBL480608 183246 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 462 4 0 4 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cc3F)CC1)C(=O)C2 10.1016/j.bmcl.2008.11.008
44570141 183492 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 488 5 1 5 2.9 CC(=O)NC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C 10.1016/j.bmcl.2008.11.008
CHEMBL482370 183492 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assayAntagonist activity at human recombinant CXCR3 receptor expressed in CHO-K1 cells assessed as human IP10-induced calcium flux by FLIPR assay
ChEMBL 488 5 1 5 2.9 CC(=O)NC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C 10.1016/j.bmcl.2008.11.008
56673944 63932 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 497 5 1 4 4.3 CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 10.1016/j.bmcl.2011.06.070
CHEMBL1809039 63932 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 497 5 1 4 4.3 CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 10.1016/j.bmcl.2011.06.070
89725952 144947 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 601 5 1 9 4.5 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCN(C)CC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3914555 144947 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 601 5 1 9 4.5 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCN(C)CC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
56680570 63900 0 None 3 2 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 438 2 2 2 4.8 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809003 63900 0 None 3 2 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 438 2 2 2 4.8 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 10.1016/j.bmcl.2011.06.070
56663560 63913 0 None 1 2 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 444 2 2 2 4.4 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(F)c2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809016 63913 0 None 1 2 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 444 2 2 2 4.4 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(F)c2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
56673944 63932 0 None -1 3 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 497 5 1 4 4.3 CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 10.1016/j.bmcl.2011.06.070
CHEMBL1809039 63932 0 None -1 3 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 497 5 1 4 4.3 CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 10.1016/j.bmcl.2011.06.070
56673945 63933 0 None 1 3 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 523 5 1 4 4.8 O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809040 63933 0 None 1 3 Mouse 8.7 pIC50 = 8.7 Functional
Antagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at mouse CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 523 5 1 4 4.8 O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
168270807 189454 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 532 6 0 10 3.5 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5172053 189454 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 532 6 0 10 3.5 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
168282215 190351 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 531 6 0 9 4.1 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4ccccc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5185762 190351 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 531 6 0 9 4.1 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4ccccc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
168280397 190686 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 495 6 0 9 3.3 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5190681 190686 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 495 6 0 9 3.3 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
117739802 151392 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 586 7 2 10 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00676
CHEMBL3966250 151392 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 586 7 2 10 3.6 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00676
89726497 152572 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 587 5 2 9 4.1 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCNCC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3976317 152572 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 587 5 2 9 4.1 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCNCC5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
53322509 57900 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 489 6 1 5 4.3 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681868 57900 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 489 6 1 5 4.3 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
168281055 190407 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 509 6 0 9 3.6 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)cc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5186627 190407 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 509 6 0 9 3.6 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)cc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
53317276 57902 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 557 7 1 5 5.9 C[C@H]1CN(c2ncc(C(=O)NCC3CCCCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
CHEMBL1681870 57902 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 557 7 1 5 5.9 C[C@H]1CN(c2ncc(C(=O)NCC3CCCCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
89726129 153017 3 None 1288 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 586 5 1 11 4.0 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3980161 153017 3 None 1288 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 586 5 1 11 4.0 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
89726463 153570 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 542 4 2 8 3.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 10.1021/acs.jmedchem.2c00676
CHEMBL3985006 153570 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 542 4 2 8 3.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 10.1021/acs.jmedchem.2c00676
12207 272 5 None -7 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assayAntagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
87056189 272 5 None -7 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assayAntagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
CHEMBL5202301 272 5 None -7 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assayAntagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
117739228 144839 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 546 6 1 8 4.0 Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C 10.1021/acs.jmedchem.2c00676
CHEMBL3913741 144839 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 546 6 1 8 4.0 Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C 10.1021/acs.jmedchem.2c00676
12207 272 5 None -7 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
87056189 272 5 None -7 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
CHEMBL5202301 272 5 None -7 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
89726538 152204 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 560 4 1 8 4.8 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00676
CHEMBL3973196 152204 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 560 4 1 8 4.8 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00676
89726625 151939 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 536 4 1 8 3.9 C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
CHEMBL3971056 151939 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 536 4 1 8 3.9 C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
45784923 5582 18 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 605 9 0 7 6.1 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077819 5582 18 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 605 9 0 7 6.1 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
46883306 5589 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 597 9 1 7 5.2 CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077826 5589 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 597 9 1 7 5.2 CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
46883307 5590 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 625 9 0 7 5.8 CCOc1ccc(-n2c([C@@H](C)N(CC3CCN(C)CC3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077827 5590 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 625 9 0 7 5.8 CCOc1ccc(-n2c([C@@H](C)N(CC3CCN(C)CC3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
44455870 154976 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 604 9 0 6 6.7 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL404201 154976 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 604 9 0 6 6.7 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
53319881 57898 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 501 6 1 5 4.9 C[C@H]1CN(c2ncc(NC(=O)C3CC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
CHEMBL1681866 57898 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 501 6 1 5 4.9 C[C@H]1CN(c2ncc(NC(=O)C3CC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
44453616 94722 0 None 8 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 495 8 1 6 4.7 CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccn1 10.1016/j.bmcl.2008.02.049
CHEMBL255798 94722 0 None 8 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 495 8 1 6 4.7 CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccn1 10.1016/j.bmcl.2008.02.049
44453558 94989 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 6 1 6 6.2 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@@H]1CCCN(C(=O)c2cccc3cccnc23)C1 10.1016/j.bmcl.2008.02.049
CHEMBL257038 94989 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 6 1 6 6.2 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@@H]1CCCN(C(=O)c2cccc3cccnc23)C1 10.1016/j.bmcl.2008.02.049
44453583 97473 0 None 4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 6 1 6 6.2 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC1CCCN(C(=O)c2cccc3cccnc23)C1 10.1016/j.bmcl.2008.02.049
CHEMBL272522 97473 0 None 4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 6 1 6 6.2 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC1CCCN(C(=O)c2cccc3cccnc23)C1 10.1016/j.bmcl.2008.02.049
44453640 97486 0 None 4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 524 9 1 6 5.3 COc1ccccc1C(=O)N(C)CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21 10.1016/j.bmcl.2008.02.049
CHEMBL272558 97486 0 None 4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 524 9 1 6 5.3 COc1ccccc1C(=O)N(C)CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21 10.1016/j.bmcl.2008.02.049
44453470 154776 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 7 1 6 6.4 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC[C@@H]1CCCN1C(=O)c1cccc2cccnc12 10.1016/j.bmcl.2008.02.049
CHEMBL403040 154776 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 7 1 6 6.4 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC[C@@H]1CCCN1C(=O)c1cccc2cccnc12 10.1016/j.bmcl.2008.02.049
44453530 154814 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 6 1 6 6.2 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@H]1CCCN(C(=O)c2cccc3cccnc23)C1 10.1016/j.bmcl.2008.02.049
CHEMBL403290 154814 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 571 6 1 6 6.2 N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@H]1CCCN(C(=O)c2cccc3cccnc23)C1 10.1016/j.bmcl.2008.02.049
44453643 158319 0 None 10 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 494 8 1 5 5.3 CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccc1 10.1016/j.bmcl.2008.02.049
CHEMBL409499 158319 0 None 10 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 494 8 1 5 5.3 CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccc1 10.1016/j.bmcl.2008.02.049
44453585 165928 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 545 8 1 6 5.8 CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1cccc2cccnc12 10.1016/j.bmcl.2008.02.049
CHEMBL427833 165928 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 545 8 1 6 5.8 CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1cccc2cccnc12 10.1016/j.bmcl.2008.02.049
56667007 63912 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 444 2 2 2 4.4 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809015 63912 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 444 2 2 2 4.4 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
168270807 189454 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 532 6 0 10 3.5 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5172053 189454 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 532 6 0 10 3.5 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
45484739 195622 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CXCR3 receptor expressed in Ba/F3 cells assessed as hMIG-induced chemotaxisAntagonist activity at recombinant human CXCR3 receptor expressed in Ba/F3 cells assessed as hMIG-induced chemotaxis
ChEMBL 558 9 1 7 4.2 N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2009.07.020
CHEMBL568676 195622 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CXCR3 receptor expressed in Ba/F3 cells assessed as hMIG-induced chemotaxisAntagonist activity at recombinant human CXCR3 receptor expressed in Ba/F3 cells assessed as hMIG-induced chemotaxis
ChEMBL 558 9 1 7 4.2 N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2009.07.020
11296495 72385 15 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of CXCL10 (IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL10 (IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 615 8 3 4 6.1 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL199839 72385 15 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of CXCL10 (IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL10 (IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 615 8 3 4 6.1 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
44453364 160037 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 460 8 1 5 4.5 CN(Cc1ccccc1)C(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 10.1016/j.bmcl.2008.02.049
CHEMBL411273 160037 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 460 8 1 5 4.5 CN(Cc1ccccc1)C(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 10.1016/j.bmcl.2008.02.049
44253168 7260 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 469 9 1 4 4.3 O=C(NCC1CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1086236 7260 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 469 9 1 4 4.3 O=C(NCC1CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
56667006 63909 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 472 2 4 4 2.6 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)[C@@H](O)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1809012 63909 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 472 2 4 4 2.6 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)[C@@H](O)C1 10.1016/j.bmcl.2011.06.070
44406196 72351 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 599 8 3 4 5.6 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL199698 72351 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 599 8 3 4 5.6 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.09.020
44580860 187421 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 498 7 0 4 4.4 COCCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O 10.1016/j.bmcl.2008.07.115
CHEMBL497396 187421 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 498 7 0 4 4.4 COCCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O 10.1016/j.bmcl.2008.07.115
46890727 7061 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 507 9 0 5 5.6 O=[N+]([O-])c1cccc(Cc2ccc(CN(Cc3ccccn3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 10.1016/j.bmcl.2010.04.113
CHEMBL1085327 7061 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 507 9 0 5 5.6 O=[N+]([O-])c1cccc(Cc2ccc(CN(Cc3ccccn3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 10.1016/j.bmcl.2010.04.113
53318514 57879 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 489 4 1 5 3.6 CNC(=O)c1cnc(N2CCN(C3CCN(C(=O)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681845 57879 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 489 4 1 5 3.6 CNC(=O)c1cnc(N2CCN(C3CCN(C(=O)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
24739388 187228 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 491 5 1 3 3.9 NS(=O)(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL495940 187228 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 491 5 1 3 3.9 NS(=O)(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
168293706 191566 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 519 5 2 8 3.3 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(=O)O)n1 10.1021/acs.jmedchem.2c00676
CHEMBL5203982 191566 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 519 5 2 8 3.3 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(=O)O)n1 10.1021/acs.jmedchem.2c00676
44406362 135216 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 497 7 3 4 4.0 CCNC(=O)N1CCCN(c2ccc(C(=O)NCC3CC3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL373008 135216 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 497 7 3 4 4.0 CCNC(=O)N1CCCN(c2ccc(C(=O)NCC3CC3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
46890726 7271 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 462 8 0 3 5.7 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(Cc2ccccc2)cc1)Cc1ccccn1 10.1016/j.bmcl.2010.04.113
CHEMBL1086280 7271 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 462 8 0 3 5.7 O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(Cc2ccccc2)cc1)Cc1ccccn1 10.1016/j.bmcl.2010.04.113
56673939 63906 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 470 2 2 3 4.3 CC1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC(C)O1 10.1016/j.bmcl.2011.06.070
CHEMBL1809009 63906 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 470 2 2 3 4.3 CC1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC(C)O1 10.1016/j.bmcl.2011.06.070
15604776 133082 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 485 6 3 4 4.0 CCNC(=O)N1CCCN(c2ccc(C(=O)NC(C)C)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL371298 133082 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 485 6 3 4 4.0 CCNC(=O)N1CCCN(c2ccc(C(=O)NC(C)C)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
46883311 5593 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 634 11 0 8 4.9 CCOc1ccc(-n2c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077830 5593 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 634 11 0 8 4.9 CCOc1ccc(-n2c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
53317277 57903 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 573 6 1 5 6.1 C[C@H]1CN(c2ncc(C(=O)Nc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
CHEMBL1681871 57903 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 573 6 1 5 6.1 C[C@H]1CN(c2ncc(C(=O)Nc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2010.12.114
56663559 63910 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 3 3 3.2 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2011.06.070
CHEMBL1809013 63910 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 442 2 3 3 3.2 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2011.06.070
45486533 195961 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 635 8 0 7 6.1 C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL570858 195961 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 635 8 0 7 6.1 C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.07.021
45486556 195997 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 645 10 0 9 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
CHEMBL571081 195997 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 645 10 0 9 4.4 CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2009.07.021
46883298 5581 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 620 10 0 7 6.6 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077818 5581 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 620 10 0 7 6.6 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
53326434 57884 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 619 7 1 5 6.8 C[C@@H]1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ncc(C(=O)NCc2ccc(Cl)c(Cl)c2)cc1Cl 10.1016/j.bmcl.2010.12.114
CHEMBL1681852 57884 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 619 7 1 5 6.8 C[C@@H]1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ncc(C(=O)NCc2ccc(Cl)c(Cl)c2)cc1Cl 10.1016/j.bmcl.2010.12.114
168290369 191319 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 607 5 1 10 3.6 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)c(F)c4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL5200180 191319 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 607 5 1 10 3.6 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)c(F)c4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
56670454 63926 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 440 3 2 2 3.9 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
CHEMBL1809033 63926 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assayAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
ChEMBL 440 3 2 2 3.9 O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccccc2)C1)N1CCCC1 10.1016/j.bmcl.2011.06.070
12207 272 5 None -7 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
87056189 272 5 None -7 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
CHEMBL5202301 272 5 None -7 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 534 4 0 9 3.6 C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 10.1021/acs.jmedchem.2c00675
34747495 6737 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 498 9 1 4 4.6 O=C(NC[C@@H]1CCCO1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083928 6737 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 498 9 1 4 4.6 O=C(NC[C@@H]1CCCO1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
46883300 5583 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 605 9 0 7 6.1 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cnccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL1077820 5583 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 605 9 0 7 6.1 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cnccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
53321187 57914 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 517 7 1 5 4.9 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C(C)C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
CHEMBL1681883 57914 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CXCR3Antagonist activity at human CXCR3
ChEMBL 517 7 1 5 4.9 CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C(C)C)C2)c(Cl)c1 10.1016/j.bmcl.2010.12.114
117739351 147939 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 536 4 1 6 5.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 10.1021/acs.jmedchem.2c00676
CHEMBL3938074 147939 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysisAntagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
ChEMBL 536 4 1 6 5.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 10.1021/acs.jmedchem.2c00676
168273685 189797 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 531 6 0 9 4.1 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cnccc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5177520 189797 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 531 6 0 9 4.1 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cnccc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
44453295 97269 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 446 7 1 5 4.2 CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)c1ccccc1 10.1016/j.bmcl.2008.02.049
CHEMBL271459 97269 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPRAntagonist activity at human CXCR3 expressed in CHO cell membrane assessed as inhibition of calcium flux by FLIPR
ChEMBL 446 7 1 5 4.2 CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)c1ccccc1 10.1016/j.bmcl.2008.02.049
24739387 187574 0 None 9 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL498556 187574 0 None 9 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
46891424 6727 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 431 7 1 7 2.5 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083913 6727 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 431 7 1 7 2.5 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccn2)cc1 10.1016/j.bmcl.2010.04.113
46891538 6338 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 448 7 1 6 3.3 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccc2F)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1082361 6338 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 448 7 1 6 3.3 N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccc2F)cc1 10.1016/j.bmcl.2010.04.113
89726522 148913 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 515 6 1 9 3.2 C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
CHEMBL3945976 148913 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 515 6 1 9 3.2 C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 10.1021/acs.jmedchem.2c00675
117739568 144194 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 504 4 1 8 3.7 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3908818 144194 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 504 4 1 8 3.7 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
46891145 7153 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 530 9 1 3 6.2 O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1085740 7153 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 530 9 1 3 6.2 O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
89726129 153017 3 None 1288 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 586 5 1 11 4.0 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
CHEMBL3980161 153017 3 None 1288 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 586 5 1 11 4.0 Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 10.1021/acs.jmedchem.2c00676
168269773 189468 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 546 6 0 8 3.6 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)CN3C(=O)Cc4ccccc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5172352 189468 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assayAntagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
ChEMBL 546 6 0 8 3.6 CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)CN3C(=O)Cc4ccccc43)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
24957182 152979 37 None 63 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 603 10 0 8 5.8 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
CHEMBL397983 152979 37 None 63 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasmaAntagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
ChEMBL 603 10 0 8 5.8 CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 10.1016/j.bmcl.2009.07.032
71525884 132283 0 None -41 4 Human 6.6 pIC50 = 6.6 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 523 8 3 10 2.6 COC(=O)[C@H]1CCCN1C(=O)c1cccc(Nc2c(N[C@@H](c3ccc(C)o3)C3(C)COC3)c(=O)c2=O)c1O nan
CHEMBL3701188 132283 0 None -41 4 Human 6.6 pIC50 = 6.6 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 523 8 3 10 2.6 COC(=O)[C@H]1CCCN1C(=O)c1cccc(Nc2c(N[C@@H](c3ccc(C)o3)C3(C)COC3)c(=O)c2=O)c1O nan
15604938 132274 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 617 8 3 4 5.7 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL370064 132274 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 617 8 3 4 5.7 CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2005.09.020
15560447 192666 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 376 4 1 3 3.6 Cc1ccc(CN2CCC(C3(c4ccccc4)CCC(=O)NC3=O)CC2)cc1 10.1016/j.bmcl.2008.07.115
CHEMBL523900 192666 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 376 4 1 3 3.6 Cc1ccc(CN2CCC(C3(c4ccccc4)CCC(=O)NC3=O)CC2)cc1 10.1016/j.bmcl.2008.07.115
168288302 190775 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 528 4 1 6 4.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 10.1021/acs.jmedchem.2c00676
CHEMBL5192187 190775 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 528 4 1 6 4.5 C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 10.1021/acs.jmedchem.2c00676
44253170 7154 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 563 11 1 5 5.6 O=C(NCCc1cccc([N+](=O)[O-])c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1085741 7154 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 563 11 1 5 5.6 O=C(NCCc1cccc([N+](=O)[O-])c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
117739438 143318 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 491 4 1 8 3.7 Cc1nnc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)o1 10.1021/acs.jmedchem.2c00676
CHEMBL3901607 143318 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysisAntagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
ChEMBL 491 4 1 8 3.7 Cc1nnc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)o1 10.1021/acs.jmedchem.2c00676
44237762 6562 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 531 9 1 4 5.5 O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
CHEMBL1083335 6562 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrsAntagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of IP10-induced chemotaxis after 4 hrs
ChEMBL 531 9 1 4 5.5 O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.04.113
90479922 190030 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 496 5 0 10 2.6 COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
CHEMBL5181086 190030 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 496 5 0 10 2.6 COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 10.1021/acs.jmedchem.2c00675
45486531 196637 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 653 8 0 7 6.3 C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 10.1016/j.bmcl.2009.07.021
CHEMBL576097 196637 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasmaAntagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
ChEMBL 653 8 0 7 6.3 C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 10.1016/j.bmcl.2009.07.021
24739889 188251 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 455 4 1 2 4.8 NC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL506627 188251 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challengeAntagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge
ChEMBL 455 4 1 2 4.8 NC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
44406274 134724 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 567 7 3 4 5.4 CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
CHEMBL372528 134724 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5Inhibition of CXCL11-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5
ChEMBL 567 7 3 4 5.4 CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.09.020
15605073 134744 0 None