Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name
GPCRdb
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ligand
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Type

Activity
Type
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Activity
Value
p-value
(-log)
Fold
selectivity
Tested
GPCRs
Assay
Description
Source

Mol
weight
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Smiles

DOI

1327 496 None 0 Human Functional pIC50 None 7.3 7.3 -6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11705773
13339 1207 None 7 Human Functional pKB = 9.5 9.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 38628803
146361282 1207 None 7 Human Functional pKB = 9.5 9.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 38628803
CHEMBL5414447 1207 None 7 Human Functional pKB = 9.5 9.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 38628803
13339 1207 None 7 Rat Functional pKB = 9.6 9.6 1 3
UnclassifiedUnclassified
Guide to Pharmacology 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 38628803
146361282 1207 None 7 Rat Functional pKB = 9.6 9.6 1 3
UnclassifiedUnclassified
Guide to Pharmacology 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 38628803
CHEMBL5414447 1207 None 7 Rat Functional pKB = 9.6 9.6 1 3
UnclassifiedUnclassified
Guide to Pharmacology 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 38628803




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page 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

146361194 195888 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 644 8 1 7 5.4 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5412684 195888 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 644 8 1 7 5.4 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
146361194 195888 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 644 8 1 7 5.4 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5412684 195888 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 644 8 1 7 5.4 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
146361364 196958 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 630 8 2 7 5.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCNC2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5435583 196958 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 630 8 2 7 5.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCNC2)n1 10.1021/acsmedchemlett.3c00514
146361364 196958 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 630 8 2 7 5.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCNC2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5435583 196958 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 630 8 2 7 5.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)N[C@@H]2CCNC2)n1 10.1021/acsmedchemlett.3c00514
146361184 196809 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 632 10 1 7 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5432648 196809 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 632 10 1 7 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)n1 10.1021/acsmedchemlett.3c00514
146361278 195987 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 642 8 1 7 5.3 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C34CCC(C(F)(F)F)(CC3)CC4)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5414709 195987 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 642 8 1 7 5.3 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C34CCC(C(F)(F)F)(CC3)CC4)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
146361184 196809 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 632 10 1 7 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5432648 196809 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 632 10 1 7 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)n1 10.1021/acsmedchemlett.3c00514
146361278 195987 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 642 8 1 7 5.3 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C34CCC(C(F)(F)F)(CC3)CC4)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5414709 195987 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 642 8 1 7 5.3 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C34CCC(C(F)(F)F)(CC3)CC4)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
146361317 195981 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 618 10 2 7 4.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5414552 195981 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 618 10 2 7 4.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)n1 10.1021/acsmedchemlett.3c00514
146361317 195981 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 618 10 2 7 4.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5414552 195981 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 618 10 2 7 4.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)n1 10.1021/acsmedchemlett.3c00514
146361372 195079 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 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 10.1021/acsmedchemlett.3c00514
CHEMBL5396357 195079 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 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 10.1021/acsmedchemlett.3c00514
146361372 195079 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 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 10.1021/acsmedchemlett.3c00514
CHEMBL5396357 195079 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 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 10.1021/acsmedchemlett.3c00514
146361524 196119 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 649 10 1 6 6.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1F 10.1021/acsmedchemlett.3c00514
CHEMBL5417272 196119 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 649 10 1 6 6.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1F 10.1021/acsmedchemlett.3c00514
146361526 196478 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 617 10 2 6 5.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5424729 196478 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 617 10 2 6 5.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)c1 10.1021/acsmedchemlett.3c00514
146361524 196119 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 649 10 1 6 6.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1F 10.1021/acsmedchemlett.3c00514
CHEMBL5417272 196119 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 649 10 1 6 6.0 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1F 10.1021/acsmedchemlett.3c00514
146361526 196478 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 617 10 2 6 5.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5424729 196478 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 617 10 2 6 5.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCNC)c1 10.1021/acsmedchemlett.3c00514
146361312 194974 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 603 9 2 6 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5394322 194974 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 603 9 2 6 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
146361312 194974 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 603 9 2 6 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5394322 194974 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 603 9 2 6 5.2 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
146361710 195578 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 587 8 1 6 4.7 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 10.1021/acsmedchemlett.3c00514
CHEMBL5406402 195578 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 587 8 1 6 4.7 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 10.1021/acsmedchemlett.3c00514
146361710 195578 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 587 8 1 6 4.7 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 10.1021/acsmedchemlett.3c00514
CHEMBL5406402 195578 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 587 8 1 6 4.7 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 10.1021/acsmedchemlett.3c00514
146361256 196050 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 631 10 1 6 5.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5415832 196050 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 631 10 1 6 5.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1 10.1021/acsmedchemlett.3c00514
146361487 195337 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5401503 195337 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
146361256 196050 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 631 10 1 6 5.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5415832 196050 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 631 10 1 6 5.9 CCOc1ncccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN(C)C)c1 10.1021/acsmedchemlett.3c00514
172470186 197101 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 601 8 1 6 5.1 CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5438739 197101 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 601 8 1 6 5.1 CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
146361487 195337 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5401503 195337 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3C(F)(F)F)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
172470186 197101 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 601 8 1 6 5.1 CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5438739 197101 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 601 8 1 6 5.1 CCOc1ccccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
13339 1207 None 7 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
146361282 1207 None 7 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
CHEMBL5414447 1207 None 7 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
146361548 196330 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(C(F)(F)F)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5421498 196330 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(C(F)(F)F)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
146361680 196941 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 592 7 2 4 6.1 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5435301 196941 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 592 7 2 4 6.1 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
146361548 196330 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(C(F)(F)F)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5421498 196330 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 9 2 5 5.9 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(C(F)(F)F)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
13339 1207 None 7 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
146361282 1207 None 7 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
CHEMBL5414447 1207 None 7 Human Binding pKi = 8.7 8.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
146361680 196941 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 592 7 2 4 6.1 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5435301 196941 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 592 7 2 4 6.1 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
146361394 195108 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 583 7 2 5 5.3 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2C#N)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5396826 195108 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 583 7 2 5 5.3 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2C#N)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
146361394 195108 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 583 7 2 5 5.3 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2C#N)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5396826 195108 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 583 7 2 5 5.3 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2C#N)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
172445098 195410 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5403170 195410 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
172445098 195410 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5403170 195410 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 602 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)NC2CCN(C)CC2)n1 10.1021/acsmedchemlett.3c00514
146361246 196395 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 588 8 1 7 4.1 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5422885 196395 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 588 8 1 7 4.1 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
146361308 195153 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 614 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5397644 195153 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 614 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 10.1021/acsmedchemlett.3c00514
146361246 196395 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 588 8 1 7 4.1 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5422885 196395 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 588 8 1 7 4.1 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CCN(C)C2)n1 10.1021/acsmedchemlett.3c00514
146361514 196881 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 610 7 2 4 6.2 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2cccc(F)c2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5434090 196881 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 610 7 2 4 6.2 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2cccc(F)c2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
146361514 196881 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 610 7 2 4 6.2 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2cccc(F)c2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5434090 196881 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 610 7 2 4 6.2 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2cccc(F)c2Cl)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
146361308 195153 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 614 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 10.1021/acsmedchemlett.3c00514
CHEMBL5397644 195153 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 614 8 1 7 4.5 CCOc1ncccc1-c1ccc(N2CCN(C(=O)C3(C(F)(F)F)CCC3)C[C@H]2CC)c(C(=O)N[C@@H]2CN3CCC2CC3)n1 10.1021/acsmedchemlett.3c00514
146361589 195515 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 568 9 2 5 5.5 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5405192 195515 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 568 9 2 5 5.5 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
146361398 197100 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 576 7 2 4 5.6 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2F)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5438731 197100 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 576 7 2 4 5.6 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2F)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
146361589 195515 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 568 9 2 5 5.5 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
CHEMBL5405192 195515 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 568 9 2 5 5.5 CCOc1ccccc1-c1ccc(N2CCN(C(=O)c3ccc(Cl)cc3Cl)C[C@H]2CC)c(C(=O)NCCN)c1 10.1021/acsmedchemlett.3c00514
146361398 197100 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 576 7 2 4 5.6 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2F)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
CHEMBL5438731 197100 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting methodDisplacement of [[125I]-Tyr23]-ACTH (1-39) from human MC2R incubated for 1.5 hrs by Topcount scintillation counting method
ChEMBL 576 7 2 4 5.6 CC[C@@H]1CN(C(=O)c2ccc(C(F)(F)F)cc2Cl)CCN1c1ccc(-c2ccccc2F)cc1C(=O)NCCN 10.1021/acsmedchemlett.3c00514
134611880 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
16132265 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
16132265.0 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
3633 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
4931 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
CHEMBL1201610 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
DB01285 277 None 0 Mouse Binding pKd = 8.0 8.0 -2 5
NoneNone
Drug Central None None None None None
1331 278 None 0 Mouse Binding pKd = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
1332 279 None 0 Human Binding pKd None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
3037130 279 None 0 Human Binding pKd None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
CHEMBL3274101 279 None 0 Human Binding pKd None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
129627786 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
1330 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
16129617 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
16129674 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
16133751 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
16133802 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
16133802.0 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
16162116 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
3767 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
4516 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
60210072 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
6965 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
CHEMBL2103784 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
DB01284 280 None 26 Mouse Binding pKd None 9.1 9.1 10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8754753
None 220225 None 0 Human Binding pKi = 8.1 8.1 - 1
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central 4538 145 63 61 -15.2 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(O)=O None
129627786 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
1330 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
16129617 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
16129674 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
16133751 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
16133802 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
16133802.0 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
16162116 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
3767 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
4516 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
60210072 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
6965 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
CHEMBL2103784 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None
DB01284 280 None 26 Human Binding pKi = 8.1 8.1 -10 2
125I-ACTH binding in OS3 cells expressing hMC2R wild type125I-ACTH binding in OS3 cells expressing hMC2R wild type
Drug Central None None None None None