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Assay Detail

CHEMBL4026745

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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 assay
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Parathyroid hormone/parathyroid hormone-related peptide receptor (CHEMBL1793) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Potent, Protease-Resistant Agonists of the Parathyroid Hormone Receptor with Broad β Residue Distribution.
Cheloha RW, Chen B, Kumar NN, Watanabe T, Thorne RG, Li L, Gardella TJ, Gellman SH.
J Med Chem (2017) 60 : 8816 -8833
PubMed 29064243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 9.11 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3301581 ABALOPARATIDE 4.0 1 10.70
CHEMBL4098420 — — 1 10.22
CHEMBL4080397 — — 1 10.15
CHEMBL4060034 — — 1 10.10
CHEMBL4090619 — — 1 9.92
CHEMBL4088173 — — 1 9.85
CHEMBL4061182 — — 1 9.82
CHEMBL4098344 — — 1 9.77
CHEMBL4106296 — — 1 9.77
CHEMBL4074628 — — 1 9.74
CHEMBL4063722 — — 1 9.59
CHEMBL4097998 — — 1 9.57
CHEMBL4063322 — — 1 9.54
CHEMBL4106303 — — 1 9.49
CHEMBL4089035 — — 1 9.47
CHEMBL4073243 — — 1 9.47
CHEMBL4093590 — — 1 9.44
CHEMBL4090894 — — 1 9.40
CHEMBL4106300 — — 1 9.36
CHEMBL4097878 — — 1 9.32
CHEMBL4063242 — — 1 9.29
CHEMBL4059512 — — 1 9.29
CHEMBL4069902 — — 1 9.28
CHEMBL4106304 — — 1 9.19
CHEMBL4083799 — — 1 9.15
CHEMBL4106302 — — 1 9.10
CHEMBL4106301 — — 1 9.08
CHEMBL4060554 — — 1 8.95
CHEMBL4090161 — — 1 8.74
CHEMBL4106298 — — 1 8.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3301581 ABALOPARATIDE EC50 = 0.02 nM 10.70
CHEMBL4098420 — EC50 = 0.06 nM 10.22
CHEMBL4080397 — EC50 = 0.07 nM 10.15
CHEMBL4060034 — EC50 = 0.08 nM 10.10
CHEMBL4090619 — EC50 = 0.12 nM 9.92
CHEMBL4088173 — EC50 = 0.14 nM 9.85
CHEMBL4061182 — EC50 = 0.15 nM 9.82
CHEMBL4098344 — EC50 = 0.17 nM 9.77
CHEMBL4106296 — EC50 = 0.17 nM 9.77
CHEMBL4074628 — EC50 = 0.18 nM 9.74
CHEMBL4063722 — EC50 = 0.26 nM 9.59
CHEMBL4097998 — EC50 = 0.27 nM 9.57
CHEMBL4063322 — EC50 = 0.29 nM 9.54
CHEMBL4106303 — EC50 = 0.32 nM 9.49
CHEMBL4073243 — EC50 = 0.34 nM 9.47
CHEMBL4089035 — EC50 = 0.34 nM 9.47
CHEMBL4093590 — EC50 = 0.36 nM 9.44
CHEMBL4090894 — EC50 = 0.4 nM 9.40
CHEMBL4106300 — EC50 = 0.44 nM 9.36
CHEMBL4097878 — EC50 = 0.48 nM 9.32
CHEMBL4059512 — EC50 = 0.51 nM 9.29
CHEMBL4063242 — EC50 = 0.51 nM 9.29
CHEMBL4069902 — EC50 = 0.52 nM 9.28
CHEMBL4106304 — EC50 = 0.65 nM 9.19
CHEMBL4083799 — EC50 = 0.71 nM 9.15
CHEMBL4106302 — EC50 = 0.79 nM 9.10
CHEMBL4106301 — EC50 = 0.83 nM 9.08
CHEMBL4060554 — EC50 = 1.12 nM 8.95
CHEMBL4090161 — EC50 = 1.8 nM 8.74
CHEMBL4106298 — EC50 = 1.84 nM 8.73
CHEMBL4098506 — EC50 = 2.59 nM 8.59
CHEMBL4059923 — EC50 = 3.0 nM 8.52
CHEMBL4106305 — EC50 = 4.13 nM 8.38
CHEMBL4091191 — EC50 = 4.98 nM 8.30
CHEMBL4095903 — EC50 = 9.74 nM 8.01
CHEMBL4101396 — EC50 = 9.84 nM 8.01
CHEMBL4078125 — EC50 = 11.51 nM 7.94
CHEMBL4106295 — EC50 = 14.57 nM 7.84
CHEMBL4071949 — EC50 = 18.69 nM 7.73
CHEMBL4067009 — EC50 = 19.0 nM 7.72
CHEMBL4106299 — EC50 = 167.0 nM 6.78
CHEMBL4068586 — EC50 - — -
CHEMBL4080315 — EC50 - — -