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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 | |
CHEMBL3092410 | 103972 | None | 0 | Human | Binding | EC50 | = | 190.00 | 6.72 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay | ChEMBL | 423.2 | 7 | 2 | 4 | 3.55 | CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 | https://dx.doi.org/10.1021/ml400275z | |
CHEMBL3092411 | 103973 | None | 0 | Human | Binding | EC50 | = | 320.00 | 6.50 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay | ChEMBL | 423.2 | 7 | 2 | 4 | 3.55 | CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 | https://dx.doi.org/10.1021/ml400275z | |
CHEMBL3092412 | 103974 | None | 0 | Human | Binding | EC50 | = | 3100.00 | 5.51 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay | ChEMBL | 443.3 | 9 | 1 | 4 | 4.10 | COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 | https://dx.doi.org/10.1021/ml400275z | |
CHEMBL5170821 | 190082 | None | 0 | Human | Binding | EC50 | = | 142.00 | 6.85 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 355.2 | 3 | 0 | 5 | 4.09 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL5170821 | 190082 | None | 0 | Human | Binding | EC50 | = | 273.00 | 6.56 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 355.2 | 3 | 0 | 5 | 4.09 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL5180932 | 190724 | None | 0 | Human | Binding | EC50 | = | 4040.00 | 5.39 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 362.2 | 6 | 1 | 5 | 2.45 | O=C(Cc1nn(CC2CCC2)c(=O)c2ccccc12)NCc1ccccn1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL5193472 | 191588 | None | 0 | Human | Binding | EC50 | = | 251.00 | 6.60 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 331.1 | 4 | 3 | 4 | 2.56 | NC(Cc1cnc[nH]1)c1nc2ccc(-c3ccccc3)cc2c(=O)[nH]1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL5195424 | 191719 | None | 0 | Human | Binding | EC50 | = | 487.00 | 6.31 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 283.2 | 4 | 2 | 5 | 3.33 | CNc1cc(-c2ccccn2)nc(NC2CCCCC2)n1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL5200611 | 192048 | None | 0 | Human | Binding | EC50 | = | 23.00 | 7.64 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 278.1 | 4 | 1 | 5 | 3.37 | CNc1nc(Oc2ccccc2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL5203229 | 192217 | None | 0 | Human | Binding | EC50 | = | 641.00 | 6.19 | - | 1 | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux | ChEMBL | 389.2 | 7 | 2 | 6 | 2.93 | Cn1cc(-c2ccc3nc(C(N)CCOCc4ccccc4)[nH]c(=O)c3c2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
compound 1 [PMID: 24900608] | 1017 | None | 3 | Human | Binding | EC50 | = | 56.00 | 7.25 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay | ChEMBL | 352.1 | 3 | 0 | 6 | 2.58 | N#Cc1ccc(N2CCN(Cc3cn4cc(Cl)ccc4n3)CC2)nc1 | https://dx.doi.org/10.1021/ml400275z |
Showing 1 to 11 of 11 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 | |
CHEMBL3092410 | 103972 | None | 0 | Human | Functional | EC50 | = | 840.00 | 6.08 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins | ChEMBL | 423.2 | 7 | 2 | 4 | 3.55 | CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 | https://dx.doi.org/10.1021/ml400275z | |
CHEMBL3092411 | 103973 | None | 0 | Human | Functional | EC50 | = | 310.00 | 6.51 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins | ChEMBL | 423.2 | 7 | 2 | 4 | 3.55 | CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 | https://dx.doi.org/10.1021/ml400275z | |
CHEMBL3092412 | 103974 | None | 0 | Human | Functional | EC50 | = | 4500.00 | 5.35 | - | 1 | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins | ChEMBL | 443.3 | 9 | 1 | 4 | 4.10 | COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 | https://dx.doi.org/10.1021/ml400275z | |
CHEMBL3198662 | 108470 | None | 8 | Human | Functional | EC50 | = | 750.00 | 6.12 | - | 1 | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay | ChEMBL | 365.2 | 8 | 5 | 9 | 2.11 | OCC(O)/C=N/Nc1nc(Nc2ccccc2)nc(Nc2ccccc2)n1 | https://dx.doi.org/10.1021/acs.jmedchem.6b00648 | |
CHEMBL3341764 | 114894 | None | 0 | Human | Functional | EC50 | = | 11.00 | 7.96 | -3 | 2 | Agonist activity at human GPR39 by IP1 assay | ChEMBL | 510.2 | 10 | 3 | 7 | 4.45 | O=S(=O)(NC[C@H]1CC[C@H](CNc2cc(-c3ccccn3)nc(NC3CC3)n2)CC1)c1cccc(F)c1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3341764 | 114894 | None | 0 | Mouse | Functional | EC50 | = | 3.00 | 8.52 | 3 | 2 | Agonist activity at mouse GPR39 by IP1 assay | ChEMBL | 510.2 | 10 | 3 | 7 | 4.45 | O=S(=O)(NC[C@H]1CC[C@H](CNc2cc(-c3ccccn3)nc(NC3CC3)n2)CC1)c1cccc(F)c1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342357 | 114999 | None | 0 | Human | Functional | EC50 | = | 202.00 | 6.70 | -50 | 2 | Agonist activity at human GPR39 by IP1 assay | ChEMBL | 510.2 | 10 | 3 | 7 | 4.45 | O=S(=O)(NC[C@H]1CC[C@H](CNc2nc(NC3CC3)cc(-c3ccccn3)n2)CC1)c1cccc(F)c1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342357 | 114999 | None | 0 | Mouse | Functional | EC50 | = | 4.00 | 8.40 | 50 | 2 | Agonist activity at mouse GPR39 by IP1 assay | ChEMBL | 510.2 | 10 | 3 | 7 | 4.45 | O=S(=O)(NC[C@H]1CC[C@H](CNc2nc(NC3CC3)cc(-c3ccccn3)n2)CC1)c1cccc(F)c1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342358 | 115000 | None | 44 | Human | Functional | EC50 | = | 0.80 | 9.10 | 2398 | 12 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 418.1 | 7 | 3 | 7 | 3.22 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342358 | 115000 | None | 44 | Human | Functional | EC50 | = | 0.80 | 9.10 | 2398 | 12 | Agonist activity at human GPR39 by IP1 assay | ChEMBL | 418.1 | 7 | 3 | 7 | 3.22 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342358 | 115000 | None | 44 | Human | Functional | EC50 | = | 0.06 | 10.22 | 2398 | 12 | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assay | ChEMBL | 418.1 | 7 | 3 | 7 | 3.22 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342358 | 115000 | None | 44 | Human | Functional | EC50 | = | 15.00 | 7.82 | 2398 | 12 | Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux | ChEMBL | 418.1 | 7 | 3 | 7 | 3.22 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1016/j.bmcl.2022.128607 | |
CHEMBL3342359 | 115001 | None | 0 | Human | Functional | EC50 | = | 164.00 | 6.79 | -1 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 255.1 | 5 | 2 | 5 | 2.40 | CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342359 | 115001 | None | 0 | Mouse | Functional | EC50 | = | 115.00 | 6.94 | 1 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 255.1 | 5 | 2 | 5 | 2.40 | CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342360 | 115002 | None | 0 | Human | Functional | EC50 | = | 5000.00 | 5.30 | -3 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 311.2 | 6 | 2 | 5 | 3.82 | CC(C)(C)CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342360 | 115002 | None | 0 | Mouse | Functional | EC50 | = | 1500.00 | 5.82 | 3 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 311.2 | 6 | 2 | 5 | 3.82 | CC(C)(C)CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342361 | 115003 | None | 0 | Human | Functional | EC50 | = | 2204.00 | 5.66 | 4 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 299.2 | 8 | 2 | 6 | 2.42 | COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342361 | 115003 | None | 0 | Mouse | Functional | EC50 | = | 10000.00 | 5.00 | -4 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 299.2 | 8 | 2 | 6 | 2.42 | COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342362 | 115004 | None | 0 | Human | Functional | EC50 | = | 600.00 | 6.22 | -27 | 2 | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 415.2 | 8 | 2 | 6 | 4.87 | FC(F)(F)Oc1ccc(CNc2nc(NCC3CC3)cc(-c3ccccn3)n2)cc1 | https://dx.doi.org/10.1021/ml500240d | |
CHEMBL3342362 | 115004 | None | 0 | Mouse | Functional | EC50 | = | 22.00 | 7.66 | 27 | 2 | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay | ChEMBL | 415.2 | 8 | 2 | 6 | 4.87 | FC(F)(F)Oc1ccc(CNc2nc(NCC3CC3)cc(-c3ccccn3)n2)cc1 | https://dx.doi.org/10.1021/ml500240d |
Showing 1 to 20 of 146 entries