Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
145705876 218107 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00876
CHEMBL3301581 218107 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00876
nan 218107 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00876
CHEMBL526530 222470 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
137659482 165962 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4098420 165962 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
134687361 164343 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4114 144 60 57 -15.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
56841901 164343 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4114 144 60 57 -15.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4080397 164343 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4114 144 60 57 -15.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137635394 162619 14 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4014 137 60 54 -14.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.7b00876
71312130 162619 14 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4014 137 60 54 -14.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.7b00876
CHEMBL4060034 162619 14 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4014 137 60 54 -14.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.7b00876
137642849 165234 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4112 142 60 57 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4090619 165234 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4112 142 60 57 -16.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137639372 166599 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at PTH1 receptor (unknown origin) assessed as induction of cAMPAgonist activity at PTH1 receptor (unknown origin) assessed as induction of cAMP
ChEMBL 4247 150 60 56 -11.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.8b00378
CHEMBL4106296 166599 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at PTH1 receptor (unknown origin) assessed as induction of cAMPAgonist activity at PTH1 receptor (unknown origin) assessed as induction of cAMP
ChEMBL 4247 150 60 56 -11.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.8b00378
137642287 165000 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4136 141 59 56 -14.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4088173 165000 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4136 141 59 56 -14.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL506126 220980 14 None -4 2 Human 9.8 pEC50 = 9.8 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
137636149 162729 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4138 143 59 56 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4061182 162729 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4138 143 59 56 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137659716 165948 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4112 142 60 57 -16.1 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4098344 165948 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4112 142 60 57 -16.1 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137639372 166599 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4247 150 60 56 -11.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
CHEMBL4106296 166599 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4247 150 60 56 -11.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
137651582 163886 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3970 128 59 53 -13.9 CC[C@H](C)[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00876
CHEMBL4074628 163886 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3970 128 59 53 -13.9 CC[C@H](C)[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00876
49841000 25349 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assayAgonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assay
ChEMBL 1346 31 17 19 -2.5 CCCC[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)COC(=O)CCCCC(=O)OC[C@@H](C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm1008264
CHEMBL1276264 25349 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assayAgonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assay
ChEMBL 1346 31 17 19 -2.5 CCCC[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)COC(=O)CCCCC(=O)OC[C@@H](C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm1008264
137634885 162930 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3995 128 58 54 -15.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4063722 162930 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3995 128 58 54 -15.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137660410 165920 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4126 143 60 57 -15.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4097998 165920 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4126 143 60 57 -15.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137637857 162902 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)C[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4063322 162902 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)C[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
129631922 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
132274287 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
132451761 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
155817470 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
16132393 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
16133850 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
4448 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
4514 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
91933454 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
CHEMBL525610 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
DB06285 10553 13 None 3 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP productionAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production
ChEMBL None None None None 10.1021/jm9018756
137657687 166605 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4089 145 60 54 -12.0 CC[C@H](C)[C@H](NC(=O)C[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)CC(N)=O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)Cc1ccccc1)CC(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4106303 166605 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4089 145 60 54 -12.0 CC[C@H](C)[C@H](NC(=O)C[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)CC(N)=O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)Cc1ccccc1)CC(C)C 10.1021/acs.jmedchem.7b00876
137640833 163776 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4097 141 59 56 -14.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4073243 163776 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4097 141 59 56 -14.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137643019 165077 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4243 147 63 55 -13.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4089035 165077 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4243 147 63 55 -13.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137654722 165519 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3982 124 58 52 -12.6 CC[C@H](C)[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00876
CHEMBL4093590 165519 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3982 124 58 52 -12.6 CC[C@H](C)[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00876
137641949 165260 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4293 143 63 55 -12.6 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCSC)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4090894 165260 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4293 143 63 55 -12.6 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCSC)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137657564 166602 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4327 153 63 55 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
CHEMBL4106300 166602 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4327 153 63 55 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
137659455 165908 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4125 127 61 53 -14.1 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4097878 165908 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4125 127 61 53 -14.1 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137636311 162564 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4075 131 61 53 -14.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4059512 162564 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4075 131 61 53 -14.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137634846 162896 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4010 123 58 52 -12.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.7b00876
CHEMBL4063242 162896 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4010 123 58 52 -12.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.7b00876
137640122 163472 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4295 145 63 55 -12.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4069902 163472 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4295 145 63 55 -12.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137657688 166606 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3998 127 59 53 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00876
CHEMBL4106304 166606 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 3998 127 59 53 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1CNC[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@H]1CCC[C@@H]1C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00876
137645140 164640 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4017 125 57 53 -14.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4083799 164640 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4017 125 57 53 -14.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137657566 166604 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4377 149 63 55 -10.2 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
CHEMBL4106302 166604 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4377 149 63 55 -10.2 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
137657565 166603 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4379 151 63 55 -10.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
CHEMBL4106301 166603 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4379 151 63 55 -10.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
44584924 200271 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
91935164 200271 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL526677 200271 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
129631922 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
132274287 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
132451761 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
155817470 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
16132393 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
16133850 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
4448 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
4514 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
91933454 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
CHEMBL525610 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
DB06285 10553 13 None 3 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL None None None None 10.1021/jm9018756
44584923 200148 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935163 200148 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL525069 200148 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL506126 220980 14 None 4 2 Rat 9.0 pEC50 = 9.0 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
137635204 162670 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CC(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C)CC(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4060554 162670 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CC(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C)CC(C)C 10.1021/acs.jmedchem.7b00876
137643296 165186 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4127 129 61 53 -13.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4090161 165186 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4127 129 61 53 -13.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137657562 166600 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4269 147 59 55 -10.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
CHEMBL4106298 166600 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4269 147 59 55 -10.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
44584918 195552 0 None -3 2 Human 6.0 pEC50 = 6 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935161 195552 0 None -3 2 Human 6.0 pEC50 = 6 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL505612 195552 0 None -3 2 Human 6.0 pEC50 = 6 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
137650056 164156 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4138 143 59 56 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4078125 164156 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4138 143 59 56 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL1276263 215453 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assayAgonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assay
ChEMBL None None None CCCC[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)CCCCNC(=O)CC[C@@H](C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm1008264
66817788 170829 6 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 517 6 2 5 2.9 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.8b00182
CHEMBL4208963 170829 6 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 517 6 2 5 2.9 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.8b00182
66817788 170829 6 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 517 6 2 5 2.9 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL4208963 170829 6 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 517 6 2 5 2.9 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.9b01743
76284228 158560 0 None - 1 Rat 4.9 pEC50 = 4.9 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 649 7 2 8 2.3 Cc1cc(N2C(=O)NC(=O)C23COC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O nan
CHEMBL3964997 158560 0 None - 1 Rat 4.9 pEC50 = 4.9 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 649 7 2 8 2.3 Cc1cc(N2C(=O)NC(=O)C23COC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O nan
CHEMBL499651 220878 0 None 3 2 Rat 6.9 pEC50 = 6.9 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL450474 220743 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
137639371 166598 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4106295 166598 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL450474 220743 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL499651 220878 0 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL514849 222375 0 None 4 2 Rat 6.8 pEC50 = 6.8 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1073/pnas.0605125104
137657563 166601 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4267 145 59 55 -10.4 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
CHEMBL4106299 166601 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4267 145 59 55 -10.4 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)CC(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(N)=O)Cc1ccccc1)C(C)C)C(C)C)Cc1c[nH]c2ccccc12 10.1021/acs.jmedchem.7b00876
137639587 163659 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4071949 163659 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137631923 163221 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4015 123 57 53 -14.3 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4067009 163221 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4015 123 57 53 -14.3 CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
76283959 158304 0 None 1 2 Rat 5.7 pEC50 = 5.7 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 661 7 2 7 3.9 Cc1cc(N2C(=O)NC(=O)C23CCCC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O nan
CHEMBL3962850 158304 0 None 1 2 Rat 5.7 pEC50 = 5.7 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 661 7 2 7 3.9 Cc1cc(N2C(=O)NC(=O)C23CCCC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O nan
CHEMBL506126 220980 14 None -4 2 Human 8.7 pEC50 = 8.7 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL1276262 215452 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assayAgonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(N)=O 10.1021/jm1008264
129631922 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
132274287 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
132451761 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
155817470 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
16132393 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
16133850 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
4448 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
4514 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
91933454 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
CHEMBL525610 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
DB06285 10553 13 None 3 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
155536792 178968 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 4115 144 60 57 -15.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)NC(Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)NC(CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)C(C)C 10.1021/acs.jmedchem.9b01743
CHEMBL4473665 178968 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 4115 144 60 57 -15.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)NC(Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)NC(CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C)C(C)C 10.1021/acs.jmedchem.9b01743
137659489 165969 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@@H](CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4098506 165969 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@@H](CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C 10.1021/acs.jmedchem.7b00876
44584923 200148 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935163 200148 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL525069 200148 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
66818600 157915 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 593 7 2 7 2.2 Cc1cc(N2C(=O)CNC2=O)ccc1CCS(=O)(=O)N1CCC2(CC1)N=C(c1cccc(OC(F)(F)F)c1)NC2=O nan
CHEMBL3959465 157915 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 593 7 2 7 2.2 Cc1cc(N2C(=O)CNC2=O)ccc1CCS(=O)(=O)N1CCC2(CC1)N=C(c1cccc(OC(F)(F)F)c1)NC2=O nan
12788 9791 33 None 1 2 Rat 5.6 pEC50 = 5.6 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F nan
76283707 9791 33 None 1 2 Rat 5.6 pEC50 = 5.6 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F nan
CHEMBL3976807 9791 33 None 1 2 Rat 5.6 pEC50 = 5.6 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F nan
DB14946 9791 33 None 1 2 Rat 5.6 pEC50 = 5.6 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F nan
44584918 195552 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935161 195552 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL505612 195552 0 None 3 2 Rat 6.6 pEC50 = 6.6 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL506126 220980 14 None -4 2 Human 7.6 pEC50 = 7.6 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of intracellular calcium mobilizationActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of intracellular calcium mobilization
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL499651 220878 0 None -3 2 Human 7.6 pEC50 = 7.6 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
66817107 170789 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 488 6 2 5 3.1 CC(=O)Nc1cc(C)c(CCS(=O)(=O)N2CCC3(CC2)N=C(C2CCCCC2)NC3=O)c(C)c1 10.1021/acs.jmedchem.8b00182
CHEMBL4208427 170789 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 488 6 2 5 3.1 CC(=O)Nc1cc(C)c(CCS(=O)(=O)N2CCC3(CC2)N=C(C2CCCCC2)NC3=O)c(C)c1 10.1021/acs.jmedchem.8b00182
137637950 162600 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4134 139 59 56 -14.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCSC)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4059923 162600 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4134 139 59 56 -14.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCSC)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL514849 222375 0 None -4 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL1084168 13646 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilizationAgonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization
ChEMBL 282 6 2 5 0.5 CCCCN1C(=O)C(=C(N)N)C(=O)N(CCCC)C1=O 10.1021/jm9018756
76283706 152485 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 633 7 2 7 3.1 Cc1cc(N2C(=O)NC(=O)C23CC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O nan
CHEMBL3916272 152485 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care).
ChEMBL 633 7 2 7 3.1 Cc1cc(N2C(=O)NC(=O)C23CC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O nan
66817215 177391 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 543 6 2 6 2.4 Cc1cc(N2C(=O)CNC2=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL4450877 177391 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 543 6 2 6 2.4 Cc1cc(N2C(=O)CNC2=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.9b01743
66817553 179301 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 531 7 2 5 3.3 CC[C@H]1CC[C@H](C2=NC3(CCN(S(=O)(=O)CCc4c(C)cc(N(C)C(N)=O)cc4C)CC3)C(=O)N2)CC1 10.1021/acs.jmedchem.9b01743
CHEMBL4483577 179301 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 531 7 2 5 3.3 CC[C@H]1CC[C@H](C2=NC3(CCN(S(=O)(=O)CCc4c(C)cc(N(C)C(N)=O)cc4C)CC3)C(=O)N2)CC1 10.1021/acs.jmedchem.9b01743
CHEMBL450474 220743 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formationActivity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells assessed as cAMP formation
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
76283959 158304 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 661 7 2 7 3.9 Cc1cc(N2C(=O)NC(=O)C23CCCC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL3962850 158304 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 661 7 2 7 3.9 Cc1cc(N2C(=O)NC(=O)C23CCCC3)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
155533095 178599 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 581 7 2 6 3.0 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL4468503 178599 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 581 7 2 6 3.0 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
137657689 166607 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4042 148 61 55 -13.1 CC[C@H](C)[C@H](NC(=O)C[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)CC(N)=O)[C@@H](C)O)CC(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4106305 166607 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4042 148 61 55 -13.1 CC[C@H](C)[C@H](NC(=O)C[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](CCCCN)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](C)CC(N)=O)[C@@H](C)O)CC(C)C 10.1021/acs.jmedchem.7b00876
44270511 175814 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4269 148 58 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\F)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL439458 175814 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4269 148 58 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\F)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
137642401 165289 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4091191 165289 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
12788 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 10.1021/acs.jmedchem.9b01743
76283707 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 10.1021/acs.jmedchem.9b01743
CHEMBL3976807 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 10.1021/acs.jmedchem.9b01743
DB14946 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 10.1021/acs.jmedchem.9b01743
155513348 176520 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 607 7 2 7 2.5 Cc1cc(N2C(=O)CNC2=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL4438541 176520 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 607 7 2 7 2.5 Cc1cc(N2C(=O)CNC2=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
155553639 180961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 621 7 2 7 2.9 Cc1cc(N2C(=O)NC(=O)C2C)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL4547545 180961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 621 7 2 7 2.9 Cc1cc(N2C(=O)NC(=O)C2C)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
44270512 172603 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4257 147 58 57 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\Cl)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL424859 172603 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4257 147 58 57 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\Cl)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
145975286 170353 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 474 6 2 5 2.8 CC(=O)Nc1ccc(CCS(=O)(=O)N2CCC3(CC2)N=C(C2CCCCC2)NC3=O)c(C)c1 10.1021/acs.jmedchem.8b00182
CHEMBL4203200 170353 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 474 6 2 5 2.8 CC(=O)Nc1ccc(CCS(=O)(=O)N2CCC3(CC2)N=C(C2CCCCC2)NC3=O)c(C)c1 10.1021/acs.jmedchem.8b00182
44584918 195552 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935161 195552 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL505612 195552 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayActivity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assay
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
155542161 179854 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 649 7 1 7 3.7 Cc1cc(N2C(=O)N(C)C(=O)C2(C)C)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
CHEMBL4519810 179854 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAAgonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
ChEMBL 649 7 1 7 3.7 Cc1cc(N2C(=O)N(C)C(=O)C2(C)C)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)NC2=O 10.1021/acs.jmedchem.9b01743
145964425 171183 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 503 6 2 5 2.6 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(C1CCCCC1)NC2=O 10.1021/acs.jmedchem.8b00182
CHEMBL4213349 171183 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayAgonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay
ChEMBL 503 6 2 5 2.6 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C(C1CCCCC1)NC2=O 10.1021/acs.jmedchem.8b00182
44584924 200271 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
91935164 200271 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL526677 200271 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
44270419 105319 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4285 148 58 57 -13.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\Cl)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL276472 105319 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4285 148 58 57 -13.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\Cl)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL514849 222375 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formationActivity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells assessed as cAMP formation
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1073/pnas.0605125104
44270513 173683 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4241 147 58 57 -14.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\F)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL428635 173683 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP productionPartial agonist activity at human PTH receptor expressed in OK-1 cells assessed as increase in cAMP production
ChEMBL 4241 147 58 57 -14.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\F)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
137652688 165728 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4094 141 60 56 -15.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4095903 165728 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4094 141 60 56 -15.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
137660321 166242 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)C[C@@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
CHEMBL4101396 166242 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayAgonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assay
ChEMBL 4128 145 60 57 -15.4 CC[C@H](C)[C@H](NC(=O)C[C@@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(C)C)C(C)C 10.1021/acs.jmedchem.7b00876
168280381 198056 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 580 6 1 6 6.0 COC1(CNC2CCOCC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
CHEMBL5190633 198056 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 580 6 1 6 6.0 COC1(CNC2CCOCC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
168289815 198081 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 608 6 1 7 5.8 COC(=O)C1(CNC2CCOCC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
CHEMBL5191139 198081 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 608 6 1 7 5.8 COC(=O)C1(CNC2CCOCC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
155536860 179023 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 434 6 2 5 4.9 COc1ccc2c(c1)N(c1ccc(NCCN)cc1)C(=O)C(C)(C)N=C2C1CCCCC1 10.1016/j.bmcl.2019.07.052
CHEMBL4474255 179023 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 434 6 2 5 4.9 COc1ccc2c(c1)N(c1ccc(NCCN)cc1)C(=O)C(C)(C)N=C2C1CCCCC1 10.1016/j.bmcl.2019.07.052
155540108 179698 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 452 6 2 4 5.8 CC(C)C1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4516490 179698 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 452 6 2 4 5.8 CC(C)C1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
168280823 198013 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 622 7 2 6 6.5 COC1(CN[C@H]2CC[C@@H](C(=O)O)CC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
CHEMBL5189957 198013 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 622 7 2 6 6.5 COC1(CN[C@H]2CC[C@@H](C(=O)O)CC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
156020093 184968 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 504 6 2 5 5.8 Cc1cnc2c(c1)-c1ccc(Cl)cc1N(c1ccc(NCCNC3CCOCC3)cc1)C(=O)C2(C)C 10.1016/j.bmc.2020.115524
CHEMBL4649331 184968 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 504 6 2 5 5.8 Cc1cnc2c(c1)-c1ccc(Cl)cc1N(c1ccc(NCCNC3CCOCC3)cc1)C(=O)C2(C)C 10.1016/j.bmc.2020.115524
155560902 181765 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 452 5 2 4 5.9 CC1(C2=NC(C)(C)C(=O)N(c3ccc(NCCN)cc3)c3cc(Cl)ccc32)CCCCC1 10.1016/j.bmcl.2019.07.052
CHEMBL4566470 181765 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 452 5 2 4 5.9 CC1(C2=NC(C)(C)C(=O)N(c3ccc(NCCN)cc3)c3cc(Cl)ccc32)CCCCC1 10.1016/j.bmcl.2019.07.052
168268911 196782 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 624 6 2 5 7.2 CC1(C)C(=O)N(c2ccc(N3CC(F)(CN[C@H]4CC[C@@](C)(C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5171324 196782 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 624 6 2 5 7.2 CC1(C)C(=O)N(c2ccc(N3CC(F)(CN[C@H]4CC[C@@](C)(C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
156020029 184877 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 524 6 2 5 6.2 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2020.115524
CHEMBL4647898 184877 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 524 6 2 5 6.2 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2020.115524
168280823 198664 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 622 7 2 6 6.5 COC1(CN[C@H]2CC[C@H](C(=O)O)CC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
CHEMBL5199789 198664 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 622 7 2 6 6.5 COC1(CN[C@H]2CC[C@H](C(=O)O)CC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
155559611 181661 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 590 8 2 7 4.8 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCN(S(C)(=O)=O)CC3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4563935 181661 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 590 8 2 7 4.8 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCN(S(C)(=O)=O)CC3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
156012452 184124 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 523 6 2 4 6.8 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2cc(Cl)ccc21 10.1016/j.bmc.2020.115524
CHEMBL4637465 184124 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 523 6 2 4 6.8 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2cc(Cl)ccc21 10.1016/j.bmc.2020.115524
155547998 180471 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 511 7 2 5 6.7 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCCCC3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4535424 180471 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 511 7 2 5 6.7 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCCCC3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
168288732 198174 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 594 6 2 6 5.7 CC1(C)C(=O)N(c2ccc(N3CC(CNC4CCOCC4)(C(=O)O)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5192509 198174 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 594 6 2 6 5.7 CC1(C)C(=O)N(c2ccc(N3CC(CNC4CCOCC4)(C(=O)O)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
155558265 181515 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 412 6 2 4 5.0 CC(C)CC1=NC(C)(C)C(=O)N(c2ccc(NCCN)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2019.07.052
CHEMBL4560415 181515 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 412 6 2 4 5.0 CC(C)CC1=NC(C)(C)C(=O)N(c2ccc(NCCN)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2019.07.052
156009840 183860 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 508 6 2 5 5.7 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(F)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2020.115524
CHEMBL4633101 183860 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 508 6 2 5 5.7 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(F)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2020.115524
156015472 184395 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 520 7 2 6 5.5 COc1ccc2c(c1)N(c1ccc(NCCNC3CCOCC3)cc1)C(=O)C(C)(C)c1ncc(Cl)cc1-2 10.1016/j.bmc.2020.115524
CHEMBL4640934 184395 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 520 7 2 6 5.5 COc1ccc2c(c1)N(c1ccc(NCCNC3CCOCC3)cc1)C(=O)C(C)(C)c1ncc(Cl)cc1-2 10.1016/j.bmc.2020.115524
168283337 197559 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 550 5 1 5 6.2 CC1(C)C(=O)N(c2ccc(N3CC(CNC4CCOCC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5183438 197559 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 550 5 1 5 6.2 CC1(C)C(=O)N(c2ccc(N3CC(CNC4CCOCC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
156022092 184983 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 489 6 2 4 6.1 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2ccccc21 10.1016/j.bmc.2020.115524
CHEMBL4649605 184983 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 489 6 2 4 6.1 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2ccccc21 10.1016/j.bmc.2020.115524
155522420 177443 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 438 5 2 4 5.5 CC1(C)N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4451534 177443 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 438 5 2 4 5.5 CC1(C)N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
156016878 184521 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 504 6 2 5 5.8 Cc1ccc2c(c1)N(c1ccc(NCCNC3CCOCC3)cc1)C(=O)C(C)(C)c1ncc(Cl)cc1-2 10.1016/j.bmc.2020.115524
CHEMBL4642502 184521 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 504 6 2 5 5.8 Cc1ccc2c(c1)N(c1ccc(NCCNC3CCOCC3)cc1)C(=O)C(C)(C)c1ncc(Cl)cc1-2 10.1016/j.bmc.2020.115524
155543526 181060 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 410 5 2 4 4.8 NCCNc1ccc(N2C(=O)CN=C(C3CCCCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2019.07.052
CHEMBL4549673 181060 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 410 5 2 4 4.8 NCCNc1ccc(N2C(=O)CN=C(C3CCCCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2019.07.052
168269753 196804 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 592 6 2 5 6.7 CC1(C)C(=O)N(c2ccc(N3CC(CN[C@H]4CC[C@@H](C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5171680 196804 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 592 6 2 5 6.7 CC1(C)C(=O)N(c2ccc(N3CC(CN[C@H]4CC[C@@H](C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
155555773 181166 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 430 5 1 5 4.7 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(OCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4552110 181166 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 430 5 1 5 4.7 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(OCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
155550447 181746 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 443 6 2 5 5.1 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4565999 181746 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 443 6 2 5 5.1 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
23582761 184341 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 538 8 2 6 6.2 CC(C)N1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCNC3CCOCC3)cn2)C1=O 10.1016/j.bmc.2020.115524
CHEMBL4640405 184341 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 538 8 2 6 6.2 CC(C)N1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCNC3CCOCC3)cn2)C1=O 10.1016/j.bmc.2020.115524
155551285 180716 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 453 6 2 5 4.6 CN(C)C1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4541000 180716 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 453 6 2 5 4.6 CN(C)C1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
155557308 181331 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 432 5 2 4 5.0 CC1(C)N=C(c2ccccc2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4556218 181331 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 432 5 2 4 5.0 CC1(C)N=C(c2ccccc2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
168269753 198151 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 592 6 2 5 6.7 CC1(C)C(=O)N(c2ccc(N3CC(CN[C@H]4CC[C@H](C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5192194 198151 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 592 6 2 5 6.7 CC1(C)C(=O)N(c2ccc(N3CC(CN[C@H]4CC[C@H](C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
16220269 196439 0 None 1 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of DPC-AJ1951-induced cAMP productionAntagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of DPC-AJ1951-induced cAMP production
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
CHEMBL515170 196439 0 None 1 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of DPC-AJ1951-induced cAMP productionAntagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of DPC-AJ1951-induced cAMP production
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
155526572 177942 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 418 5 2 4 5.2 Cc1ccc2c(c1)N(c1ccc(NCCN)cc1)C(=O)C(C)(C)N=C2C1CCCCC1 10.1016/j.bmcl.2019.07.052
CHEMBL4458800 177942 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 418 5 2 4 5.2 Cc1ccc2c(c1)N(c1ccc(NCCN)cc1)C(=O)C(C)(C)N=C2C1CCCCC1 10.1016/j.bmcl.2019.07.052
155518374 177069 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 466 6 2 4 6.2 CC(C)C1(C)N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4446377 177069 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 466 6 2 4 6.2 CC(C)C1(C)N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
16220269 196439 0 None 1 5 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of parathyroid hormone (1 to 34)-induced cAMP productionAntagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of parathyroid hormone (1 to 34)-induced cAMP production
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
CHEMBL515170 196439 0 None 1 5 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of parathyroid hormone (1 to 34)-induced cAMP productionAntagonist activity at PTH/PTH-related peptide receptor expressed in HKRK-B28 cells assessed as inhibition of parathyroid hormone (1 to 34)-induced cAMP production
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
155546261 180307 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 429 5 2 5 4.8 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4531282 180307 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 429 5 2 5 4.8 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
155522839 177572 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 428 5 1 4 5.3 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(CCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4453102 177572 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 428 5 1 4 5.3 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(CCCN)cc2)C1=O 10.1016/j.bmcl.2019.07.052
168290054 198082 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 594 6 0 6 6.3 COC1(CN(C)C2CCOCC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
CHEMBL5191156 198082 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 594 6 0 6 6.3 COC1(CN(C)C2CCOCC2)CN(c2ccc(N3C(=O)C(C)(C)c4ncc(Cl)cc4-c4ccc(Cl)cc43)cc2)C1 10.1016/j.bmc.2022.116763
12004 8270 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 610 6 2 5 6.8 Clc1cc2c(C(C(=O)N(c3c2ccc(c3)Cl)c2ccc(cc2)N2CC(C2)(F)CNC2CCC(CC2)C(=O)O)(C)C)nc1 10.1016/j.bmc.2022.116763
163358786 8270 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 610 6 2 5 6.8 Clc1cc2c(C(C(=O)N(c3c2ccc(c3)Cl)c2ccc(cc2)N2CC(C2)(F)CNC2CCC(CC2)C(=O)O)(C)C)nc1 10.1016/j.bmc.2022.116763
CHEMBL5201424 8270 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 610 6 2 5 6.8 Clc1cc2c(C(C(=O)N(c3c2ccc(c3)Cl)c2ccc(cc2)N2CC(C2)(F)CNC2CCC(CC2)C(=O)O)(C)C)nc1 10.1016/j.bmc.2022.116763
156014618 183970 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 508 6 2 5 5.7 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2cc(F)cnc21 10.1016/j.bmc.2020.115524
CHEMBL4635077 183970 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 508 6 2 5 5.7 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(Cl)ccc2-c2cc(F)cnc21 10.1016/j.bmc.2020.115524
168280840 197502 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 566 5 2 6 5.3 CC1(C)C(=O)N(c2ccc(N3CC(O)(CNC4CCOCC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5182497 197502 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 566 5 2 6 5.3 CC1(C)C(=O)N(c2ccc(N3CC(O)(CNC4CCOCC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
168290134 198257 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 582 6 2 5 6.0 CC1(C)C(=O)N(c2ccc(N3CC(F)(CN[C@H]4C[C@H](C(=O)O)C4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5193454 198257 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 582 6 2 5 6.0 CC1(C)C(=O)N(c2ccc(N3CC(F)(CN[C@H]4C[C@H](C(=O)O)C4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
156009701 183949 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 512 7 2 5 6.4 CC1(C)C=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmc.2020.115524
CHEMBL4634580 183949 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 512 7 2 5 6.4 CC1(C)C=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmc.2020.115524
168291743 198788 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 636 6 2 5 7.3 CC1(C)C(=O)N(c2ccc(N3CC(F)(CNC45CCC(C(=O)O)(CC4)CC5)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5201635 198788 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 636 6 2 5 7.3 CC1(C)C(=O)N(c2ccc(N3CC(F)(CNC45CCC(C(=O)O)(CC4)CC5)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
168268911 198815 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 624 6 2 5 7.2 CC1(C)C(=O)N(c2ccc(N3CC(F)(CN[C@H]4CC[C@](C)(C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
CHEMBL5202067 198815 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assayAntagonist activity against human PTHR1 expressed in CHO-K1 cells assessed as reduction in PTH induced cAMP level incubated for 30 mins in presence of IBMX by cAMP assay
ChEMBL 624 6 2 5 7.2 CC1(C)C(=O)N(c2ccc(N3CC(F)(CN[C@H]4CC[C@](C)(C(=O)O)CC4)C3)cc2)c2cc(Cl)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2022.116763
139035050 178366 16 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 513 7 2 6 5.6 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmc.2020.115524
CHEMBL4465123 178366 16 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 513 7 2 6 5.6 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmc.2020.115524
156016201 184480 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 515 6 2 6 5.4 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(C#N)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2020.115524
CHEMBL4642072 184480 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 515 6 2 6 5.4 CC1(C)C(=O)N(c2ccc(NCCNC3CCOCC3)cc2)c2cc(C#N)ccc2-c2cc(Cl)cnc21 10.1016/j.bmc.2020.115524
139035050 178366 16 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 513 7 2 6 5.6 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4465123 178366 16 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 513 7 2 6 5.6 CC1(C)N=C(C2CCCCC2)c2ccc(C#N)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
25118026 178621 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 477 5 1 4 6.2 CC(C)N1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(CC3=NCCN3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
CHEMBL4468837 178621 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assayAntagonist activity at human PTHR1 expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 477 5 1 4 6.2 CC(C)N1N=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(CC3=NCCN3)cc2)C1=O 10.1016/j.bmcl.2019.07.052
156018523 184560 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 521 7 2 4 7.2 CC1(C)C=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmc.2020.115524
CHEMBL4643152 184560 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 minsAntagonist activity at PTHR1 (unknown origin) expressed in CHOK1 cells co-expressing Gs/Gq assessed as reduction in human PTH (1 to 34 residues)-induced cAMP level incubated for 30 mins
ChEMBL 521 7 2 4 7.2 CC1(C)C=C(C2CCCCC2)c2ccc(Cl)cc2N(c2ccc(NCCNC3CCOCC3)cc2)C1=O 10.1016/j.bmc.2020.115524
23626557 99077 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant PTH1 receptor expressed in HEK293 cells assessed as inhibition of PTH(1-34)-stimulated cAMP productionAntagonist activity at human recombinant PTH1 receptor expressed in HEK293 cells assessed as inhibition of PTH(1-34)-stimulated cAMP production
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242784 99077 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant PTH1 receptor expressed in HEK293 cells assessed as inhibition of PTH(1-34)-stimulated cAMP productionAntagonist activity at human recombinant PTH1 receptor expressed in HEK293 cells assessed as inhibition of PTH(1-34)-stimulated cAMP production
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
23626557 99077 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human wild type PTH1 receptor expressed in SaOS2 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uMAntagonist activity at human wild type PTH1 receptor expressed in SaOS2 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uM
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242784 99077 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human wild type PTH1 receptor expressed in SaOS2 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uMAntagonist activity at human wild type PTH1 receptor expressed in SaOS2 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uM
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
23626557 99077 0 None - 0 Human 5.5 pKd = 5.5 Functional
Antagonist activity at human recombinant PTH2 receptor expressed in CHOK1 cells assessed as inhibition of TIP (1-39)-stimulated cAMP production at 10 uMAntagonist activity at human recombinant PTH2 receptor expressed in CHOK1 cells assessed as inhibition of TIP (1-39)-stimulated cAMP production at 10 uM
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242784 99077 0 None - 0 Human 5.5 pKd = 5.5 Functional
Antagonist activity at human recombinant PTH2 receptor expressed in CHOK1 cells assessed as inhibition of TIP (1-39)-stimulated cAMP production at 10 uMAntagonist activity at human recombinant PTH2 receptor expressed in CHOK1 cells assessed as inhibition of TIP (1-39)-stimulated cAMP production at 10 uM
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
23626557 99077 0 None - 0 Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse wild type PTH1 receptor expressed in MC3T3E1 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uMAntagonist activity at mouse wild type PTH1 receptor expressed in MC3T3E1 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uM
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242784 99077 0 None - 0 Mouse 6.3 pKd = 6.3 Functional
Antagonist activity at mouse wild type PTH1 receptor expressed in MC3T3E1 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uMAntagonist activity at mouse wild type PTH1 receptor expressed in MC3T3E1 cells assessed as inhibition of PTHrP (1-34)-stimulated cAMP production at 3 uM
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
12788 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 32022560
76283707 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 32022560
CHEMBL3976807 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 32022560
DB14946 9791 33 None -1 2 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 635 7 2 7 3.3 O=C1NC(=NC12CCN(S(=O)(CCC3=C(C=C(N4C(NC(C4(C)C)=O)=O)C=C3C)C)=O)CC2)C5=CC=C(C=C5)OC(F)(F)F 32022560
129631922 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
132274287 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
132451761 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
155817470 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
16132393 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
16133850 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
4448 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
4514 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
91933454 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
CHEMBL525610 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
DB06285 10553 13 None 3 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
129631922 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
132274287 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
132451761 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
155817470 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
16132393 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
16133850 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
4448 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
4514 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
91933454 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
CHEMBL525610 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
DB06285 10553 13 None -3 4 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
145705876 224526 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 3958 142 61 55 -15.4 CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(N)=O None
5576 7120 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18946036
5575 7117 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18946036
12004 8270 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 610 6 2 5 6.8 Clc1cc2c(C(C(=O)N(c3c2ccc(c3)Cl)c2ccc(cc2)N2CC(C2)(F)CNC2CCC(CC2)C(=O)O)(C)C)nc1 35487102
163358786 8270 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 610 6 2 5 6.8 Clc1cc2c(C(C(=O)N(c3c2ccc(c3)Cl)c2ccc(cc2)N2CC(C2)(F)CNC2CCC(CC2)C(=O)O)(C)C)nc1 35487102
CHEMBL5201424 8270 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 610 6 2 5 6.8 Clc1cc2c(C(C(=O)N(c3c2ccc(c3)Cl)c2ccc(cc2)N2CC(C2)(F)CNC2CCC(CC2)C(=O)O)(C)C)nc1 35487102
129631922 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
132274287 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
132451761 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
155817470 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
16132393 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
16133850 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
4448 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
4514 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
91933454 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
CHEMBL525610 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
DB06285 10553 13 None 3 4 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
155817432 10007 0 None 70 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
16144017 10007 0 None 70 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1822 10007 0 None 70 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
155817433 10600 0 None 12 3 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11046116
16134968 10600 0 None 12 3 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11046116
1827 10600 0 None 12 3 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11046116
5574 7118 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18946036
5573 7119 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18946036
1794 8711 0 None -31 3 Rat 5.1 pIC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1794 8711 0 None -19 3 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1793 8710 0 None - 1 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
155817428 10008 0 None 6 2 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1790 10008 0 None 6 2 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1815 10598 0 None -31 3 Human 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10854439
1815 10598 0 None -31 3 Human 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1821 8783 0 None 1 2 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
1807 9878 0 None 5 2 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1808 10644 0 None -2 2 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9360953
155817430 10599 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1816 10599 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
129316189 10003 0 None -15 3 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
155817471 10003 0 None -15 3 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
16201228 10003 0 None -15 3 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
4449 10003 0 None -15 3 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
155817429 10009 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11046116
1814 10009 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11046116
1813 10667 0 None - 1 Human 7.3 pIC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1809 10643 0 None -1 2 Human 7.3 pIC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1819 8280 0 None 3 2 Human 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11046116
1795 8775 0 None - 1 Rat 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1804 8778 0 None - 1 Human 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1801 8782 0 None 3 2 Human 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
155817431 10602 0 None - 1 Human 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
16200083 10602 0 None - 1 Human 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1818 10602 0 None - 1 Human 7.4 pIC50 None 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1797 8785 0 None -1 2 Human 7.5 pIC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9360953
1798 8779 0 None 1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
1798 8779 0 None 1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1799 8780 0 None 1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
155817427 10006 0 None 1 3 Human 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
1788 10006 0 None 1 3 Human 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702701
155817426 10005 0 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1787 10005 0 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
1800 8781 0 None 3 2 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10537121
1802 8786 0 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1812 10666 0 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8662729
1796 8774 0 None - 1 Rat 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1806 9604 0 None - 1 Rat 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8662729
1805 9603 0 None - 1 Rat 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8662729
1811 10665 0 None - 1 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8662729
1810 10664 0 None - 1 Human 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159842
129631922 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
132274287 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
132451761 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
155817470 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
16132393 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
16133850 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
4448 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
4514 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
91933454 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
CHEMBL525610 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
DB06285 10553 13 None -3 4 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1803 8776 0 None - 1 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796
1792 7257 0 None - 1 Rat 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7896796




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
129631922 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
132274287 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
132451761 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
155817470 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
16132393 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
16133850 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
4448 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
4514 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
91933454 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
CHEMBL525610 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
DB06285 10553 13 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.8b00182
44584918 195552 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935161 195552 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL505612 195552 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 2135 66 27 27 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL514849 222375 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL450474 220743 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
44584924 200271 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
91935164 200271 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL526677 200271 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 1980 59 25 25 -0.4 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL499651 220878 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL506126 220980 14 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells in presence of SW106Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells in presence of SW106
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL506126 220980 14 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
CHEMBL526530 222470 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
66817788 170829 6 None - 0 Human 4.0 pIC50 = 4.0 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL 517 6 2 5 2.9 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.8b00182
CHEMBL4208963 170829 6 None - 0 Human 4.0 pIC50 = 4.0 Binding
Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisDisplacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis
ChEMBL 517 6 2 5 2.9 Cc1cc(N(C)C(N)=O)cc(C)c1CCS(=O)(=O)N1CCC2(CC1)N=C([C@H]1CC[C@H](C)CC1)NC2=O 10.1021/acs.jmedchem.8b00182
44584923 200148 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
91935163 200148 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
CHEMBL525069 200148 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 2108 65 27 27 -0.7 CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12)C(N)=O 10.1073/pnas.0605125104
16220269 196439 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
CHEMBL515170 196439 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsDisplacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL 361 3 1 2 4.4 CC[C@@H]1O[C@](/C=C/C2CC2)(C(F)(F)F)c2c(ccc(F)c2F)NC1=O 10.1073/pnas.0605125104
44270419 105319 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4285 148 58 57 -13.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\Cl)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL276472 105319 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4285 148 58 57 -13.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\Cl)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
44270512 172603 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4257 147 58 57 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\Cl)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL424859 172603 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4257 147 58 57 -14.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\Cl)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
44270511 175814 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4269 148 58 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\F)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL439458 175814 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4269 148 58 57 -13.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](/C=C(\F)[C@H](C)N)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL506126 220980 14 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to PTH/PTH-related peptide receptor expressed in HKRK-B28 cellsBinding affinity to PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1073/pnas.0605125104
44270513 173683 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4241 147 58 57 -14.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\F)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
CHEMBL428635 173683 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to human PTH receptor expressed in OK-1 cellsBinding affinity to human PTH receptor expressed in OK-1 cells
ChEMBL 4241 147 58 57 -14.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C)/C=C(\F)[C@H](C)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C)C(C)C 10.1021/acs.jmedchem.7b01788
11963968 99910 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 586 7 2 4 8.2 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1CCc3ccccc3CC1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL244325 99910 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 586 7 2 4 8.2 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1CCc3ccccc3CC1)N=C2C1CCCCC1 10.1021/jm0707626
23626730 150158 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 561 9 3 5 7.5 Cc1cc2c(cc1NCc1ccccc1)C(C1CCCCC1)=NN(C)C(=O)N2c1ccc(NCCc2ncc[nH]2)cc1 10.1021/jm0707626
CHEMBL389783 150158 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 561 9 3 5 7.5 Cc1cc2c(cc1NCc1ccccc1)C(C1CCCCC1)=NN(C)C(=O)N2c1ccc(NCCc2ncc[nH]2)cc1 10.1021/jm0707626
23626731 150166 1 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 562 9 2 5 7.4 Cc1cc2c(cc1OCc1ccccc1)C(C1CCCCC1)=NN(C)C(=O)N2c1ccc(NCCc2ncc[nH]2)cc1 10.1021/jm0707626
CHEMBL389787 150166 1 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 562 9 2 5 7.4 Cc1cc2c(cc1OCc1ccccc1)C(C1CCCCC1)=NN(C)C(=O)N2c1ccc(NCCc2ncc[nH]2)cc1 10.1021/jm0707626
44428092 156818 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 537 7 2 4 7.0 Cc1ccc2c(c1)N(c1ccc(NC(=O)C(N)C(C)C)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL395054 156818 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 537 7 2 4 7.0 Cc1ccc2c(c1)N(c1ccc(NC(=O)C(N)C(C)C)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
23626557 99077 0 None 8 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242784 99077 0 None 8 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 456 6 2 4 5.9 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
23626400 99076 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 480 5 3 3 6.4 Cc1ccc2c(c1)N(c1ccc(NC(=N)N)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242778 99076 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 480 5 3 3 6.4 Cc1ccc2c(c1)N(c1ccc(NC(=N)N)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
23626559 151199 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 470 7 2 4 6.3 Cc1ccc2c(c1)N(c1ccc(NCCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL390628 151199 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 470 7 2 4 6.3 Cc1ccc2c(c1)N(c1ccc(NCCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
23626097 98953 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 466 5 3 3 6.1 N=C(N)Nc1cccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)c1 10.1021/jm0707626
CHEMBL242391 98953 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 466 5 3 3 6.1 N=C(N)Nc1cccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)c1 10.1021/jm0707626
23626399 98998 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 492 5 2 5 6.1 O=C1N(Cc2ccccc2)N=C(C2CCCCC2)c2ccccc2N1c1ccc(NC2=NCCN2)cc1 10.1021/jm0707626
CHEMBL242590 98998 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 492 5 2 5 6.1 O=C1N(Cc2ccccc2)N=C(C2CCCCC2)c2ccccc2N1c1ccc(NC2=NCCN2)cc1 10.1021/jm0707626
23626561 99580 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 484 7 2 4 6.6 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C(C)C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL243698 99580 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 484 7 2 4 6.6 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C(C)C)N=C2C1CCCCC1 10.1021/jm0707626
23626403 98983 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 532 8 2 4 7.4 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL242567 98983 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 532 8 2 4 7.4 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
23626240 100037 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 460 5 3 3 5.5 N=C(N)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(c3ccccc3)c3ccccc32)cc1 10.1021/jm0707626
CHEMBL244930 100037 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 460 5 3 3 5.5 N=C(N)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(c3ccccc3)c3ccccc32)cc1 10.1021/jm0707626
44428091 148826 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 523 7 2 4 6.7 CC(C)C(N)C(=O)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
CHEMBL387792 148826 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 523 7 2 4 6.7 CC(C)C(N)C(=O)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
23626558 100067 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 442 5 2 4 5.8 Cc1ccc2c(c1)N(c1ccc(NCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL245110 100067 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 442 5 2 4 5.8 Cc1ccc2c(c1)N(c1ccc(NCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCCCC1 10.1021/jm0707626
23626241 100038 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 480 6 3 3 6.4 N=C(N)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(CC3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
CHEMBL244931 100038 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 480 6 3 3 6.4 N=C(N)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(CC3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
23626891 100046 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 526 7 2 5 6.4 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1CCOCC1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL244956 100046 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 526 7 2 5 6.4 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1CCOCC1)N=C2C1CCCCC1 10.1021/jm0707626
23626732 91886 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 588 7 2 5 7.0 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1CCc3ccccc3CC1)N=C2C1CCOCC1 10.1021/jm0707626
CHEMBL224729 91886 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 588 7 2 5 7.0 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1CCc3ccccc3CC1)N=C2C1CCOCC1 10.1021/jm0707626
23626560 99717 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 484 8 2 4 6.6 CCCN1N=C(C2CCCCC2)c2ccc(C)cc2N(c2ccc(NCCc3ncc[nH]3)cc2)C1=O 10.1021/jm0707626
CHEMBL244074 99717 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 484 8 2 4 6.6 CCCN1N=C(C2CCCCC2)c2ccc(C)cc2N(c2ccc(NCCc3ncc[nH]3)cc2)C1=O 10.1021/jm0707626
23626733 99994 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 458 6 2 5 4.7 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCOCC1 10.1021/jm0707626
CHEMBL244735 99994 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 458 6 2 5 4.7 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C)N=C2C1CCOCC1 10.1021/jm0707626
23626243 98997 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 481 6 2 4 5.6 NCC(=O)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
CHEMBL242589 98997 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 481 6 2 4 5.6 NCC(=O)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
23626402 173941 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 506 5 2 5 6.4 Cc1ccc2c(c1)N(c1ccc(NC3=NCCN3)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL429099 173941 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 506 5 2 5 6.4 Cc1ccc2c(c1)N(c1ccc(NC3=NCCN3)cc1)C(=O)N(Cc1ccccc1)N=C2C1CCCCC1 10.1021/jm0707626
12001598 156115 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 466 5 3 3 6.1 N=C(N)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
CHEMBL394513 156115 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 466 5 3 3 6.1 N=C(N)Nc1ccc(N2C(=O)N(Cc3ccccc3)N=C(C3CCCCC3)c3ccccc32)cc1 10.1021/jm0707626
23626734 149144 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 590 7 2 6 7.1 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1COc3ccccc3OC1)N=C2C1CCCCC1 10.1021/jm0707626
CHEMBL388911 149144 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 590 7 2 6 7.1 Cc1ccc2c(c1)N(c1ccc(NCCc3ncc[nH]3)cc1)C(=O)N(C1COc3ccccc3OC1)N=C2C1CCCCC1 10.1021/jm0707626
23626894 148827 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 500 9 2 5 5.9 COCCN1N=C(C2CCCCC2)c2ccc(C)cc2N(c2ccc(NCCc3ncc[nH]3)cc2)C1=O 10.1021/jm0707626
CHEMBL387793 148827 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 500 9 2 5 5.9 COCCN1N=C(C2CCCCC2)c2ccc(C)cc2N(c2ccc(NCCc3ncc[nH]3)cc2)C1=O 10.1021/jm0707626
44428090 149143 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 556 7 3 3 7.6 N=C(N)Nc1ccc(Cc2ccc(N3C(=O)N(Cc4ccccc4)N=C(C4CCCCC4)c4ccccc43)cc2)cc1 10.1021/jm0707626
CHEMBL388909 149143 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellsDisplacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cells
ChEMBL 556 7 3 3 7.6 N=C(N)Nc1ccc(Cc2ccc(N3C(=O)N(Cc4ccccc4)N=C(C4CCCCC4)c4ccccc43)cc2)cc1 10.1021/jm0707626