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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 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Binding | IC50 | = | 10.00 | 8.00 | - | 2 | Antagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP binding | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Binding | IC50 | = | 1.00 | 9.00 | - | 2 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3908230 | 144746 | None | 2 | Human | Binding | IC50 | = | 50.12 | 7.30 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 518.1 | 8 | 2 | 8 | 2.68 | CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3908230 | 144746 | None | 2 | Human | Binding | IC50 | = | 53.00 | 7.28 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 518.1 | 8 | 2 | 8 | 2.68 | CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3923733 | 146755 | None | 0 | Human | Binding | IC50 | = | 15.85 | 7.80 | - | 2 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3926111 | 147048 | None | 0 | Human | Binding | IC50 | = | 501.19 | 6.30 | - | 2 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 483.1 | 7 | 2 | 4 | 4.11 | CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3933303 | 147963 | None | 0 | Human | Binding | IC50 | = | 79.43 | 7.10 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 457.2 | 7 | 2 | 6 | 2.56 | Cc1ccc(S(=O)(=O)NC(CCn2cccc2C#N)C(=O)N2CCC(C)CC2)c(C)c1N | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3943972 | 149293 | None | 0 | Human | Binding | IC50 | = | 1258.93 | 5.90 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 474.1 | 7 | 2 | 7 | 2.16 | CC1CCN(C(=O)C(CCn2nccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3948828 | 149917 | None | 0 | Human | Binding | IC50 | = | 1258.93 | 5.90 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 473.1 | 7 | 2 | 6 | 2.77 | CC1CCN(C(=O)C(CCn2cccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3951018 | 150192 | None | 0 | Human | Binding | IC50 | = | 15.85 | 7.80 | - | 2 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 497.1 | 7 | 2 | 6 | 3.24 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3951018 | 150192 | None | 0 | Human | Binding | IC50 | = | 3.16 | 8.50 | - | 2 | Displacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysis | ChEMBL | 497.1 | 7 | 2 | 6 | 3.24 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3951018 | 150192 | None | 0 | Human | Binding | IC50 | = | 19.95 | 7.70 | - | 2 | Antagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP binding | ChEMBL | 497.1 | 7 | 2 | 6 | 3.24 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3951018 | 150192 | None | 0 | Human | Binding | IC50 | = | 3.40 | 8.47 | - | 2 | Reversible inhibition of human CCL27-Fc binding to CCR10 expressed in HEK cell membranes by immunochemical binding assay | ChEMBL | 497.1 | 7 | 2 | 6 | 3.24 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3951018 | 150192 | None | 0 | Human | Binding | IC50 | = | 3.40 | 8.47 | - | 2 | Displacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysis | ChEMBL | 497.1 | 7 | 2 | 6 | 3.24 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3964547 | 151822 | None | 0 | Human | Binding | IC50 | = | 251.19 | 6.60 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 507.1 | 7 | 2 | 6 | 3.42 | CC1CCN(C(=O)C(CCn2ccnc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3971886 | 152678 | None | 0 | Human | Binding | IC50 | = | 12.59 | 7.90 | - | 1 | Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3[nH]ccc3c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 |
Showing 1 to 16 of 16 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 | |
BI-6901 | 629 | None | 0 | Human | Functional | pIC50 | = | - | 9.00 | 25 | 2 | Unclassified | Guide to Pharmacology | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)[C@@H](CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://pubmed.ncbi.nlm.nih.gov/27692854 | |
BI-6901 | 629 | None | 0 | Mouse | Functional | pIC50 | = | - | 7.60 | -25 | 2 | Unclassified | Guide to Pharmacology | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)[C@@H](CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://pubmed.ncbi.nlm.nih.gov/27692854 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 1.26 | 8.90 | 42 | 2 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 1.00 | 9.00 | 42 | 2 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 25.12 | 7.60 | 42 | 2 | Antagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP production | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 2.00 | 8.70 | 42 | 2 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 1.00 | 9.00 | 42 | 2 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 3162.28 | 5.50 | 42 | 2 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Human | Functional | IC50 | = | 0.40 | 9.40 | 42 | 2 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Mouse | Functional | IC50 | = | 63.10 | 7.20 | -42 | 2 | Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Mouse | Functional | IC50 | = | 25.12 | 7.60 | -42 | 2 | Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3889627 | 142475 | None | 1 | Mouse | Functional | IC50 | = | 15848.93 | 4.80 | -42 | 2 | Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3890608 | 142596 | None | 0 | Human | Functional | IC50 | = | 63.10 | 7.20 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 453.2 | 7 | 2 | 5 | 2.84 | CC1CCCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)C1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3891289 | 142677 | None | 0 | Human | Functional | IC50 | = | 125.89 | 6.90 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 517.1 | 7 | 2 | 4 | 4.77 | CC1CCN(C(=O)C(CCc2ccccc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3891692 | 142730 | None | 0 | Human | Functional | IC50 | = | 10.00 | 8.00 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 507.2 | 7 | 2 | 5 | 3.38 | N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCC(C(F)(F)F)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3896799 | 143356 | None | 0 | Human | Functional | IC50 | = | 1258.93 | 5.90 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 414.2 | 7 | 1 | 5 | 2.35 | CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccccc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3901006 | 143869 | None | 0 | Human | Functional | IC50 | = | 251.19 | 6.60 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 497.1 | 7 | 2 | 6 | 3.39 | N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCCCCC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3904154 | 144270 | None | 0 | Human | Functional | IC50 | = | 7.94 | 8.10 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 497.1 | 7 | 2 | 6 | 3.24 | CC1CCN(C(=O)[C@@H](CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3908230 | 144746 | None | 2 | Human | Functional | IC50 | = | 794.33 | 6.10 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay | ChEMBL | 518.1 | 8 | 2 | 8 | 2.68 | CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 | |
CHEMBL3908230 | 144746 | None | 2 | Human | Functional | IC50 | = | 630.96 | 6.20 | - | 1 | Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay | ChEMBL | 518.1 | 8 | 2 | 8 | 2.68 | CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2016.09.047 |
Showing 1 to 20 of 64 entries