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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
AZD3778 | 547 | None | 6 | Human | Binding | pKi | = | - | 8.20 | 1 | 2 | Assay using sodium salt of the compound | Guide to Pharmacology | 525.1 | 5 | 1 | 5 | 4.71 | Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 | https://pubmed.ncbi.nlm.nih.gov/23031591 | |
AZD3778 | 547 | None | 6 | Human | Binding | IC50 | = | 8.10 | 8.09 | 1 | 2 | Antagonist activity at CCR3 assessed as inhibition of eotaxin binding | ChEMBL | 525.1 | 5 | 1 | 5 | 4.71 | Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 | https://dx.doi.org/10.1021/jm300682j | |
AZD3778 | 547 | None | 6 | Human | Binding | Ki | = | 6.31 | 8.20 | 1 | 2 | Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay | ChEMBL | 525.1 | 5 | 1 | 5 | 4.71 | Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2012.08.124 | |
AZD3778 | 547 | None | 6 | Human | Binding | Ki | = | 6.31 | 8.20 | 1 | 2 | Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay | ChEMBL | 525.1 | 5 | 1 | 5 | 4.71 | Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2012.08.103 | |
banyu (I) | 574 | None | 5 | Human | Binding | pKi | = | - | 8.50 | - | 2 | Unclassified | Guide to Pharmacology | 480.1 | 6 | 2 | 6 | 5.06 | Nc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 | https://pubmed.ncbi.nlm.nih.gov/12450563 | |
banyu (I) | 574 | None | 5 | Human | Binding | pKd | None | - | 8.30 | - | 2 | Unclassified | Guide to Pharmacology | 480.1 | 6 | 2 | 6 | 5.06 | Nc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 | https://pubmed.ncbi.nlm.nih.gov/12450563 | |
banyu (I) | 574 | None | 5 | Human | Binding | IC50 | = | 2.30 | 8.64 | - | 2 | Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells | ChEMBL | 480.1 | 6 | 2 | 6 | 5.06 | Nc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 | https://dx.doi.org/10.1016/s0960-894x(01)00176-7 | |
banyu (I) | 574 | None | 5 | Human | Binding | IC50 | = | 2.30 | 8.64 | - | 2 | Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand | ChEMBL | 480.1 | 6 | 2 | 6 | 5.06 | Nc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1 | https://dx.doi.org/10.1016/s0960-894x(03)00748-0 | |
BERLEX COMPOUND | 118652 | None | 11 | Human | Binding | IC50 | = | 9000.00 | 5.05 | - | 4 | Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells | ChEMBL | 444.2 | 7 | 1 | 3 | 5.91 | N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 | https://dx.doi.org/10.1021/jm0201767 | |
BMS compound 87b | 692 | None | 0 | Human | Binding | pKi | = | - | 8.10 | - | 1 | Unclassified | Guide to Pharmacology | 451.3 | 10 | 3 | 4 | 4.50 | CC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 | https://pubmed.ncbi.nlm.nih.gov/12067561 | |
BMS compound 87b | 692 | None | 0 | Human | Binding | IC50 | = | 6.00 | 8.22 | - | 1 | In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin | ChEMBL | 451.3 | 10 | 3 | 4 | 4.50 | CC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 | https://dx.doi.org/10.1016/s0960-894x(02)00206-8 | |
BMS compound 87b | 692 | None | 0 | Human | Binding | IC50 | = | 8.00 | 8.10 | - | 1 | In vitro inhibition if C-C chemokine receptor type 3 (CCR3) using 150p M [125I]-labeled human eotaxin | ChEMBL | 451.3 | 10 | 3 | 4 | 4.50 | CC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 | https://dx.doi.org/10.1016/s0960-894x(02)00206-8 | |
CCL11 | 826 | None | 0 | Human | Binding | pKi | = | - | 9.75 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8642344 | |
CCL11 | 827 | None | 0 | Human | Binding | pKi | = | - | 9.85 | 446 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8642344 | |
CCL2 | 838 | None | 0 | Human | Binding | pKi | None | - | 7.50 | 1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8642344 | |
CCL5 | 865 | None | 0 | Human | Binding | pKi | = | - | 8.90 | -3 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8642344 | |
CCL7 | 866 | None | 0 | Human | Binding | pKi | = | - | 8.90 | 6 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8642344 | |
cenicriviroc | 879 | None | 32 | Human | Binding | IC50 | = | 2400.00 | 5.62 | - | 6 | Displacement of [125I]eotaxin from CCR3 expressed in CHO cells | ChEMBL | 696.4 | 17 | 1 | 7 | 8.74 | CCCCOCCOc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc([S@@](=O)Cc4cncn4CCC)cc2)CCCN3CC(C)C)cc1 | https://dx.doi.org/10.1021/jm0509703 | |
CHEMBL1180359 | 11460 | None | 0 | Human | Binding | IC50 | = | 11.00 | 7.96 | - | 1 | Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells | ChEMBL | 483.2 | 6 | 2 | 4 | 5.53 | C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccccc2)CC1 | https://dx.doi.org/10.1021/jm0201767 | |
CHEMBL1180385 | 11474 | None | 0 | Human | Binding | IC50 | = | 2.00 | 8.70 | - | 1 | Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells | ChEMBL | 501.2 | 6 | 2 | 4 | 5.67 | C[N+]1(Cc2cc3c(cc2NC(=O)Nc2cccc(C#N)c2)OCO3)CCC(Cc2ccc(F)cc2)CC1 | https://dx.doi.org/10.1021/jm0201767 |
Showing 1 to 20 of 1,100 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
AZD3778 | 547 | None | 6 | Human | Functional | Kd | = | 100.00 | 7.00 | 4 | 2 | Antagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysis | ChEMBL | 525.1 | 5 | 1 | 5 | 4.71 | Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2012.08.124 | |
BMS compound 87b | 692 | None | 0 | Human | Functional | IC50 | = | 20.00 | 7.70 | - | 1 | In vitro C-C chemokine receptor type 3 activity of compound by using eotaxin induced human eosinophil chemotaxis assay | ChEMBL | 451.3 | 10 | 3 | 4 | 4.50 | CC[C@H](O)[C@H]1C[C@@H](Cc2ccccc2)CCN1CCCNC(=O)Nc1cccc(C(C)=O)c1 | https://dx.doi.org/10.1016/s0960-894x(02)00206-8 | |
CCL11 | 827 | None | 0 | Human | Functional | pIC50 | = | - | 8.85 | 14 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9276730 | |
CCL11 | 827 | None | 0 | Human | Functional | pIC50 | = | - | 8.85 | 14 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10488147 | |
CCL11 | 827 | None | 0 | Human | Functional | pIC50 | = | - | 8.85 | 14 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16339911 | |
CCL11 | 827 | None | 0 | Human | Functional | pIC50 | = | - | 8.85 | 14 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12761559 | |
CCL11 | 827 | None | 0 | Human | Functional | pIC50 | = | - | 8.85 | 14 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10854442 | |
CCL13 | 828 | None | 0 | Human | Functional | pIC50 | = | - | 9.50 | 7 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9276730 | |
CCL13 | 828 | None | 0 | Human | Functional | pIC50 | = | - | 9.50 | 7 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16339911 | |
CCL15 | 830 | None | 0 | Human | Functional | pIC50 | = | - | 8.60 | 5 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9346309 | |
CCL18 | 833 | None | 0 | Human | Functional | pIC50 | = | - | 7.50 | 25 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/23951310 | |
CCL24 | 849 | None | 0 | Human | Functional | pIC50 | = | - | 8.70 | 316 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15207250 | |
CCL24 | 849 | None | 0 | Human | Functional | pIC50 | = | - | 8.70 | 316 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16339911 | |
CCL26 | 853 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15207250 | |
CCL26 | 853 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10488147 | |
CCL26 | 853 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16339911 | |
CHEMBL123611 | 16507 | None | 0 | Human | Functional | IC50 | = | 30.00 | 7.52 | - | 1 | Inhibition of eotaxin-induced chemotaxis of human eosinophils | ChEMBL | 516.3 | 8 | 3 | 4 | 5.49 | CNC(=O)c1cccc(NC(=O)Nc2cccc(C(C)=O)c2)c1CN1CCC(Cc2ccc(F)cc2)CC1 | https://dx.doi.org/10.1021/jm049530m | |
CHEMBL175634 | 60526 | None | 0 | Human | Functional | IC50 | = | 10.00 | 8.00 | - | 1 | Inhibition of calcium mobilization in human eosinophils | ChEMBL | 453.3 | 7 | 2 | 3 | 5.47 | COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 | https://dx.doi.org/10.1021/jm049530m | |
CHEMBL175634 | 60526 | None | 0 | Human | Functional | IC50 | = | 115.00 | 6.94 | - | 1 | Inhibition of eotaxin-induced chemotaxis of human eosinophils | ChEMBL | 453.3 | 7 | 2 | 3 | 5.47 | COc1ccccc1NC(=O)N[C@@H]1CCCC[C@H]1CN1CCC[C@@H](Cc2ccc(F)cc2)C1 | https://dx.doi.org/10.1021/jm049530m | |
CHEMBL178019 | 62507 | None | 0 | Human | Functional | IC50 | = | 350.00 | 6.46 | - | 1 | Antagonist activity against C-C chemokine receptor type 3 | ChEMBL | 461.2 | 9 | 2 | 6 | 3.28 | C=C(NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)c1cccc2ccccc12)C(=O)OCC | https://dx.doi.org/10.1016/s0960-894x(01)00249-9 |
Showing 1 to 20 of 327 entries