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Assay Detail

CHEMBL944465

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Binding
Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed in HKRK-B28 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HKRK-B28
Confidence 8 — Homologous single protein target
Curated By Intermediate

Publication

Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.
Carter PH, Liu RQ, Foster WR, Tamasi JA, Tebben AJ, Favata M, Staal A, Cvijic ME, French MH, Dell V, Apanovitch D, Lei M, Zhao Q, Cunningham M, Decicco CP, Trzaskos JM, Feyen JH.
Proc Natl Acad Sci U S A (2007) 104 : 6846 -6851
PubMed 17428923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.42 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506126 1 8.16
CHEMBL526530 1 8.14
CHEMBL526677 1 7.87
CHEMBL525069 1 7.01
CHEMBL515170 1 6.00
CHEMBL499651 1 5.66
CHEMBL505612 1 4.99
CHEMBL514849 1 4.98
CHEMBL450474 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506126 IC50 = 6.87 nM 8.16
CHEMBL526530 IC50 = 7.2 nM 8.14
CHEMBL526677 IC50 = 13.5 nM 7.87
CHEMBL525069 IC50 = 98.2 nM 7.01
CHEMBL515170 IC50 = 990.0 nM 6.00
CHEMBL499651 IC50 = 2187.0 nM 5.66
CHEMBL505612 IC50 = 10130.0 nM 4.99
CHEMBL514849 IC50 = 10484.0 nM 4.98
CHEMBL450474 IC50 = 10560.0 nM 4.98