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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 | |
| ACTH | 277 | None | 0 | Mouse | Binding | pKd | = | 9.80 | 8.01 | -2 | 5 | None | Drug Central | - | - | - | - | - | - | - | |
| ACTH | 278 | None | 0 | Mouse | Binding | pKd | = | - | 9.80 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8754753 | |
| ACTH-(1-24) | 280 | None | 26 | Human | Binding | pKi | = | 8.27 | 8.08 | -10 | 3 | 125I-ACTH binding in OS3 cells expressing hMC2R wild type | Drug Central | - | - | - | - | - | - | - | |
| ACTH-(1-24) | 280 | None | 26 | Mouse | Binding | pKd | None | - | 9.10 | 10 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8754753 | |
| ACTH-(11-24) | 279 | None | 0 | Human | Binding | pKd | None | - | 9.00 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8754753 | |
| CHEMBL5394322 | 194974 | None | 0 | Human | Binding | Ki | = | 1.26 | 8.90 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 603.2 | 9 | 2 | 6 | 5.25 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5394322 | 194974 | None | 0 | Human | Binding | Ki | = | 1.10 | 8.96 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 603.2 | 9 | 2 | 6 | 5.25 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5396357 | 195079 | None | 0 | Human | Binding | Ki | = | 0.63 | 9.20 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 602.3 | 8 | 1 | 7 | 4.53 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5396357 | 195079 | None | 0 | Human | Binding | Ki | = | 0.63 | 9.20 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 602.3 | 8 | 1 | 7 | 4.53 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5396826 | 195108 | None | 0 | Human | Binding | Ki | = | 25.12 | 7.60 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 583.2 | 7 | 2 | 5 | 5.33 | CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2C#N)cc1C(=O)NCCN | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5396826 | 195108 | None | 0 | Human | Binding | Ki | = | 25.00 | 7.60 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 583.2 | 7 | 2 | 5 | 5.33 | CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2C#N)cc1C(=O)NCCN | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5397644 | 195153 | None | 0 | Human | Binding | Ki | = | 3.98 | 8.40 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 614.3 | 8 | 1 | 7 | 4.53 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5397644 | 195153 | None | 0 | Human | Binding | Ki | = | 4.40 | 8.36 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 614.3 | 8 | 1 | 7 | 4.53 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5401503 | 195337 | None | 0 | Human | Binding | Ki | = | 1.58 | 8.80 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 602.2 | 9 | 2 | 5 | 5.85 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5401503 | 195337 | None | 0 | Human | Binding | Ki | = | 1.60 | 8.80 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 602.2 | 9 | 2 | 5 | 5.85 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5403170 | 195410 | None | 0 | Human | Binding | Ki | = | 3.16 | 8.50 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 602.3 | 8 | 1 | 7 | 4.53 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5403170 | 195410 | None | 0 | Human | Binding | Ki | = | 3.00 | 8.52 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 602.3 | 8 | 1 | 7 | 4.53 | CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5405192 | 195515 | None | 0 | Human | Binding | Ki | = | 5.01 | 8.30 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 568.2 | 9 | 2 | 5 | 5.49 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5405192 | 195515 | None | 0 | Human | Binding | Ki | = | 4.80 | 8.32 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 568.2 | 9 | 2 | 5 | 5.49 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
| CHEMBL5406402 | 195578 | None | 0 | Human | Binding | Ki | = | 1.26 | 8.90 | - | 1 | Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method | ChEMBL | 587.3 | 8 | 1 | 6 | 4.74 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 | https://dx.doi.org/10.1021/acsmedchemlett.3c00514 | |
Showing 1 to 20 of 52 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 | |
| ASIP [90-132 (L89Y)] | 496 | None | 0 | Human | Functional | pIC50 | None | - | 7.30 | -6 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11705773 | |
| CRN04894 | 1207 | None | 7 | Human | Functional | pKB | = | - | 9.47 | -1 | 3 | Unclassified | Guide to Pharmacology | 613.3 | 8 | 1 | 6 | 5.13 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 | https://pubmed.ncbi.nlm.nih.gov/38628803 | |
| CRN04894 | 1207 | None | 7 | Rat | Functional | pKB | = | - | 9.64 | 1 | 3 | Unclassified | Guide to Pharmacology | 613.3 | 8 | 1 | 6 | 5.13 | CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 | https://pubmed.ncbi.nlm.nih.gov/38628803 | |
Showing 1 to 3 of 3 entries