Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ligand		 Fold
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GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
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Description		 Source

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 DOI
71461073 84590 2 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 84590 2 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 84590 2 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 84590 2 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 139101 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 139101 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 139215 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 139215 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 139215 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 139146 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 139146 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 84538 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 84538 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 84538 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 84544 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 84544 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 84544 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 84549 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 84549 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 84549 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 84552 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 84552 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 84552 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 138996 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 138996 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 84546 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 84546 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 84546 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 84550 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 84550 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 84550 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 84555 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 84555 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 84555 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 139171 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 139171 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 139212 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 139212 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 139212 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 139078 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 139078 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 84584 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 84584 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 84584 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 139085 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 139085 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 83026 6 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 83026 6 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 83026 6 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 139096 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 139096 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 83026 6 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 83026 6 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 83026 6 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 84548 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 84548 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 84548 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 84554 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 84554 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 84554 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 83026 6 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 83026 6 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 83026 6 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 84536 2 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 84536 2 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 84536 2 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 84543 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 84543 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 84543 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 84545 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 84545 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 84545 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 139000 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 139000 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 139187 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 139187 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 139213 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 139213 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 139213 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 58221 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 58221 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 179178 6 None -4 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 179178 6 None -4 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 5670 0 None 1 5 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 5670 0 None 1 5 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 179178 6 None 2 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 179178 6 None 2 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 5670 0 None 1 5 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 5670 0 None 1 5 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 5670 0 None 1 5 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 5670 0 None 1 5 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 58221 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 58221 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 179178 6 None -2 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 179178 6 None -2 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 145884 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 145884 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 153409 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 153409 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 58221 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 58221 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 153409 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 153409 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 190995 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 190995 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 146805 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 146805 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 275 8 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 275 8 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 275 8 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 143102 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 143102 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 5663 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 5663 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 155086 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 155086 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 64224 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 64224 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 191483 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 191483 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 64224 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 64224 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 64252 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 64252 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 95400 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 95400 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 198159 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 198159 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 198423 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 198423 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 72730 22 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 72730 22 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 187921 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 187921 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 188105 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 188105 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 188156 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 188156 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 177610 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 177610 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 64258 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 64258 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 69968 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 69968 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 190766 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 190766 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 191803 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 191803 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 151978 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 151978 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 69969 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 69969 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 6830 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 6830 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 64254 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 64254 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 64251 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 64251 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 58175 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 58175 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 188157 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 188157 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 143628 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 143628 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 64234 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 64234 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 6828 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 6828 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 148768 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 148768 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 94797 1 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 94797 1 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 94797 1 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 94797 1 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 94797 1 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 94797 1 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 7274 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 7274 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 190669 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 190669 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 191726 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 191726 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 64226 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 64226 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 64242 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 64242 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 64236 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 64236 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 198553 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 198553 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 187737 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 187737 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 140572 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 140572 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 145884 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 145884 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 153661 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 153661 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 177610 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 177610 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 72616 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 72616 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 58199 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 58199 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 177605 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 177605 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 152471 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 152471 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 188091 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 188091 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 188104 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 188104 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 189539 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 189539 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 193089 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 193089 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 198557 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 198557 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 6477 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 6477 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 6634 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 6634 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 64228 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 64228 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 6423 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 6423 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 153853 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 153853 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 64229 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 64229 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 191542 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 191542 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 72594 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 72594 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 132825 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 132825 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 6178 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 6178 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 191542 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 191542 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 4651 0 None 13 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 4651 0 None 13 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 150684 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 150684 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 190243 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 190243 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 191390 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 191390 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 64229 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 64229 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 64255 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 64255 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 64227 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 64227 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 147696 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 147696 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 190808 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 190808 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 86033 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 86033 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 58217 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 58217 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 188157 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 188157 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 192474 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 192474 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 58197 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 58197 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 154104 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 154104 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 190808 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 190808 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 147119 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 147119 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 193244 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 193244 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 6479 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 6479 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 191783 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 191783 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 5670 0 None 1 5 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 5670 0 None 1 5 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 153513 44 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 153513 44 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 147036 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 147036 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 191369 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 191369 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 153513 44 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 153513 44 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 187778 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 187778 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 149267 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 149267 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 187898 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 187898 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 6414 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 6414 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 7174 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 7174 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 176705 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 176705 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 178373 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 178373 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 183065 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 183065 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 183904 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 183904 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 177585 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 177585 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 188162 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 188162 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 176570 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 176570 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 189871 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 189871 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 177586 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 177586 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 177734 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 177734 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 183826 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 183826 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 189940 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 189940 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 58190 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 58190 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 64236 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 64236 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 64243 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 64243 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 64255 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 64255 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 5668 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 5668 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 191280 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 191280 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 191719 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 191719 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 147036 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 147036 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 5656 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 5656 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 58176 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 58176 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 197610 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 197610 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 187899 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 187899 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 64260 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 64260 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 133436 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 133436 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 150873 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 150873 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 191273 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 191273 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 64232 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 64232 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 190550 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 190550 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 190685 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 190685 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 58178 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 58178 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 198925 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 198925 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 198925 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 198925 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 190669 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 190669 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 197653 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 197653 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 198527 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 198527 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 198555 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 198555 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 187839 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 187839 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 7293 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 7293 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 64225 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 64225 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 63933 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 63933 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 64242 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 64242 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 191374 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 191374 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 74153 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 74153 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 153853 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 153853 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 6635 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 6635 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 7175 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 7175 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 198290 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 198290 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 58182 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 58182 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 6816 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 6816 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 176706 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 176706 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 178728 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 178728 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 177728 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 177728 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 183905 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 183905 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 183828 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 183828 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 184074 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 184074 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 64263 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 64263 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 145480 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 145480 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 64231 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 64231 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 64244 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 64244 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 64263 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 64263 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 64264 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 64264 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 190047 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 190047 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 190945 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 190945 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 191280 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 191280 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 151924 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 151924 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 153106 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 153106 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 58208 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 58208 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 191001 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 191001 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 58210 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 58210 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 153551 4 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 153551 4 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 154104 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 154104 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 275 8 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 275 8 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 275 8 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 145372 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 145372 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 275 8 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 275 8 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 275 8 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 152736 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 152736 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 152471 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 152471 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 5658 23 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 5658 23 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 5665 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 5665 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 5666 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 5666 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 155514 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 155514 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 58206 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 58206 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 95165 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 95165 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 95433 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 95433 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 97922 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 97922 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 97935 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 97935 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 155315 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 155315 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 155353 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 155353 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 158865 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 158865 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 166481 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 166481 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 64243 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 64243 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 190047 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 190047 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 197298 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 197298 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 72730 22 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 72730 22 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 160584 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 160584 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 7341 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 7341 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 64240 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 64240 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 72696 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 72696 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 188004 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 188004 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 7140 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 7140 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 58187 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 58187 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 187811 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 187811 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 192164 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 192164 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 135739 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 135739 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 7352 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 7352 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 64237 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 64237 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 133605 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 133605 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 5669 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 5669 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 58211 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 58211 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 64241 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 64241 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 197638 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 197638 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 197674 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 197674 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 5657 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 5657 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 58192 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 58192 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 191916 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 191916 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 64257 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 64257 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 275 8 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 275 8 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 275 8 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 6815 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 6815 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 5659 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 5659 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 58222 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 58222 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 148471 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 148471 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 190391 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