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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 | |
CANDESARTAN CILEXETIL | 4402 | None | 68 | Human | Binding | AC50 | = | 21196.30 | 4.67 | - | 29 | Binding affinity towards human GIPR in an in vitro assay with cellular components measured by scintillation proximity assay | ChEMBL | 610.3 | 10 | 1 | 11 | 6.32 | CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 | https://dx.doi.org/10.1038/s41467-023-40064-9 | |
CHEMBL1933360 | 69459 | None | 0 | Human | Binding | Ki | = | 4080.00 | 5.39 | -11 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 475.2 | 10 | 2 | 5 | 5.02 | CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL1933360 | 69459 | None | 0 | Human | Binding | Ki | = | 939.00 | 6.03 | -11 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 475.2 | 10 | 2 | 5 | 5.02 | CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL1933363 | 69462 | None | 0 | Human | Binding | Ki | = | 1950.00 | 5.71 | -54 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 474.2 | 10 | 3 | 5 | 5.05 | CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL1933364 | 69463 | None | 0 | Human | Binding | Ki | = | 300.00 | 6.52 | -44 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 528.2 | 10 | 3 | 5 | 5.59 | O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL1933364 | 69463 | None | 0 | Human | Binding | Ki | = | 3840.00 | 5.42 | -44 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 528.2 | 10 | 3 | 5 | 5.59 | O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL1933365 | 69464 | None | 0 | Human | Binding | Ki | = | 927.00 | 6.03 | -30 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 500.2 | 9 | 3 | 5 | 5.44 | O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL1933365 | 69464 | None | 0 | Human | Binding | Ki | = | 152.00 | 6.82 | -30 | 3 | Displacement of [125I]GIP from human GIPR | ChEMBL | 500.2 | 9 | 3 | 5 | 5.44 | O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.10.113 | |
CHEMBL198736 | 72436 | None | 41 | Human | Binding | IC50 | = | 28.30 | 7.55 | - | 4 | Binding affinity to human cloned GIPR expressed in BHK cells | ChEMBL | 563.3 | 9 | 3 | 4 | 6.43 | CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL198736 | 72436 | None | 41 | Rat | Binding | IC50 | = | 42.00 | 7.38 | - | 4 | Binding affinity to GIPR in rat liver membrane | ChEMBL | 563.3 | 9 | 3 | 4 | 6.43 | CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL219384 | 83406 | None | 2 | Human | Binding | IC50 | = | 38.00 | 7.42 | - | 3 | Binding affinity to human cloned GIPR expressed in BHK cells | ChEMBL | 557.2 | 9 | 3 | 4 | 6.33 | CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL375167 | 137326 | None | 0 | Human | Binding | IC50 | = | 93.00 | 7.03 | - | 2 | Binding affinity to human cloned GIPR expressed in BHK cells | ChEMBL | 615.3 | 8 | 3 | 3 | 7.57 | CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL386446 | 141925 | None | 0 | Human | Binding | IC50 | = | 64.00 | 7.19 | - | 4 | Binding affinity to human cloned GIPR expressed in BHK cells | ChEMBL | 565.2 | 9 | 3 | 3 | 7.39 | O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL386446 | 141925 | None | 0 | Rat | Binding | IC50 | = | 216.00 | 6.67 | - | 4 | Binding affinity to GIPR in rat liver membrane | ChEMBL | 565.2 | 9 | 3 | 3 | 7.39 | O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL442651 | 169544 | None | 0 | Human | Binding | IC50 | = | 645.00 | 6.19 | - | 2 | Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay | ChEMBL | 613.2 | 9 | 2 | 5 | 7.94 | O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 | https://dx.doi.org/10.1021/jm8016249 | |
CHEMBL443971 | 169929 | None | 0 | Human | Binding | IC50 | = | 1002.00 | 6.00 | - | 2 | Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay | ChEMBL | 647.2 | 11 | 2 | 5 | 9.63 | O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(Cl)cc3)c(-c3ccccc3)s2)cc1 | https://dx.doi.org/10.1021/jm8016249 | |
CHEMBL444126 | 170029 | None | 0 | Human | Binding | IC50 | = | 368.00 | 6.43 | - | 2 | Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay | ChEMBL | 605.2 | 10 | 2 | 5 | 8.33 | O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 | https://dx.doi.org/10.1021/jm8016249 | |
CHEMBL445532 | 171037 | None | 0 | Human | Binding | IC50 | = | 380.00 | 6.42 | - | 2 | Binding affinity to human cloned GIPR expressed in BHK cells | ChEMBL | 659.1 | 9 | 4 | 4 | 6.84 | O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Br)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 | https://dx.doi.org/10.1021/jm7015599 | |
CHEMBL446821 | 171909 | None | 0 | Human | Binding | IC50 | = | 950.00 | 6.02 | - | 3 | Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay | ChEMBL | 581.2 | 10 | 2 | 6 | 6.74 | O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 | https://dx.doi.org/10.1021/jm8016249 | |
CHEMBL446821 | 171909 | None | 0 | Human | Binding | IC50 | = | 770.00 | 6.11 | - | 3 | Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay | ChEMBL | 581.2 | 10 | 2 | 6 | 6.74 | O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 | https://dx.doi.org/10.1021/jm8016249 |
Showing 1 to 20 of 104 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 | |
CHEMBL1643951 | 56874 | None | 0 | Human | Functional | IC50 | = | 45.00 | 7.35 | -3 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 559.3 | 7 | 3 | 6 | 5.99 | CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1643952 | 56875 | None | 0 | Human | Functional | IC50 | = | 4100.00 | 5.39 | -2 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 444.2 | 6 | 1 | 4 | 6.24 | O=C(O)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1643953 | 56876 | None | 0 | Human | Functional | IC50 | = | 2800.00 | 5.55 | 1 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 515.2 | 9 | 2 | 5 | 5.75 | O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1643954 | 56877 | None | 0 | Human | Functional | IC50 | = | 910.00 | 6.04 | -1 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 511.2 | 7 | 2 | 7 | 5.31 | O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1643955 | 56878 | None | 0 | Human | Functional | IC50 | = | 2100.00 | 5.68 | -15 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 511.2 | 7 | 2 | 7 | 5.31 | O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1644173 | 56931 | None | 0 | Human | Functional | IC50 | = | 7400.00 | 5.13 | -6 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 515.2 | 9 | 2 | 5 | 5.61 | O=C(O)CCNC(=O)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1644178 | 56936 | None | 0 | Human | Functional | IC50 | = | 5700.00 | 5.24 | -54 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 567.3 | 7 | 2 | 7 | 6.58 | CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1644182 | 56940 | None | 0 | Human | Functional | IC50 | = | 3000.00 | 5.52 | -85 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 573.1 | 7 | 2 | 7 | 6.24 | O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1644183 | 56941 | None | 0 | Human | Functional | IC50 | = | 7500.00 | 5.12 | -89 | 4 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 577.1 | 9 | 2 | 5 | 6.67 | O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1644183 | 56941 | None | 0 | Human | Functional | IC50 | = | 6277.00 | 5.20 | -89 | 4 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ChEMBL | 577.1 | 9 | 2 | 5 | 6.67 | O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 | https://dx.doi.org/10.1021/jm300579z | |
CHEMBL1644184 | 56942 | None | 0 | Human | Functional | IC50 | = | 7100.00 | 5.15 | -63 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 573.1 | 7 | 2 | 7 | 6.24 | O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1644188 | 56946 | None | 0 | Human | Functional | IC50 | = | 6000.00 | 5.22 | -14 | 2 | Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL | 603.1 | 8 | 2 | 8 | 6.39 | CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 | https://dx.doi.org/10.1016/j.bmcl.2010.11.074 | |
CHEMBL1922834 | 68984 | None | 0 | Human | Functional | IC50 | = | 370.00 | 6.43 | -81 | 3 | Inhibition of human GIP receptor by cAMP assay | ChEMBL | 634.2 | 9 | 2 | 9 | 5.73 | CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.085 | |
CHEMBL1922835 | 68985 | None | 1 | Human | Functional | IC50 | = | 510.00 | 6.29 | -40 | 3 | Inhibition of human GIP receptor by cAMP assay | ChEMBL | 600.2 | 9 | 2 | 9 | 5.37 | CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.085 | |
CHEMBL1922839 | 68989 | None | 0 | Human | Functional | IC50 | = | 290.00 | 6.54 | -54 | 3 | Inhibition of human GIP receptor by cAMP assay | ChEMBL | 606.3 | 8 | 2 | 8 | 6.13 | CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.085 | |
CHEMBL1922840 | 68990 | None | 0 | Human | Functional | IC50 | = | 1500.00 | 5.82 | -165 | 3 | Inhibition of human GIP receptor by cAMP assay | ChEMBL | 618.2 | 8 | 2 | 8 | 5.85 | CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.085 | |
CHEMBL1922841 | 68991 | None | 0 | Human | Functional | IC50 | = | 1600.00 | 5.80 | -141 | 3 | Inhibition of human GIP receptor by cAMP assay | ChEMBL | 634.2 | 9 | 2 | 9 | 5.73 | CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.085 | |
CHEMBL1922842 | 68992 | None | 0 | Human | Functional | IC50 | = | 1100.00 | 5.96 | -41 | 3 | Inhibition of human GIP receptor by cAMP assay | ChEMBL | 618.2 | 8 | 2 | 8 | 5.85 | CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.085 | |
CHEMBL1922933 | 69017 | None | 0 | Human | Functional | IC50 | = | 1400.00 | 5.85 | -128 | 2 | Antagonist activity at human GIP receptor assessed as inhibition of cAMP production | ChEMBL | 612.2 | 13 | 2 | 4 | 8.13 | CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/j.bmcl.2011.09.105 | |
CHEMBL198387 | 72344 | None | 9 | Human | Functional | IC50 | = | 430.00 | 6.37 | -7 | 3 | Inhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulation | ChEMBL | 585.3 | 6 | 2 | 6 | 6.16 | CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2005.06.101 |
Showing 1 to 20 of 100 entries