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Assay Detail

CHEMBL654539

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-salmon calcitonin (sCT) from calcitonin receptor of rat brain
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Calcitonin receptor (CHEMBL2204)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Side-chain lactam-bridge conformational constraints differentiate the activities of salmon and human calcitonins and reveal a new design concept for potent calcitonin analogues.
Taylor JW, Jin QK, Sbacchi M, Wang L, Belfiore P, Garnier M, Kazantzis A, Kapurniotu A, Zaratin PF, Scheideler MA.
J Med Chem (2002) 45 : 1108 -1121
PubMed 11855991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.03 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2369912 1 9.74
CHEMBL2369886 1 9.60
CHEMBL2369895 1 9.49
CHEMBL2369907 1 9.42
CHEMBL2369915 1 9.39
CHEMBL2369893 1 8.27
CHEMBL2369899 1 7.22
CHEMBL2369897 1 7.10
CHEMBL2369906 1 6.76
CHEMBL2304022 1 5.72
CHEMBL2369892 1 5.61
CHEMBL2369905 1 -
CHEMBL2369898 1 -
CHEMBL2369904 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2369912 IC50 = 0.18 nM 9.74
CHEMBL2369886 IC50 = 0.249 nM 9.60
CHEMBL2369895 IC50 = 0.326 nM 9.49
CHEMBL2369907 IC50 = 0.377 nM 9.42
CHEMBL2369915 IC50 = 0.408 nM 9.39
CHEMBL2369893 IC50 = 5.39 nM 8.27
CHEMBL2369899 IC50 = 60.0 nM 7.22
CHEMBL2369897 IC50 = 79.0 nM 7.10
CHEMBL2369906 IC50 = 173.0 nM 6.76
CHEMBL2304022 IC50 = 1905.0 nM 5.72
CHEMBL2369892 IC50 = 2450.0 nM 5.61
CHEMBL2369905 IC50 > 5000.0 nM -
CHEMBL2369898 IC50 > 5000.0 nM -
CHEMBL2369904 IC50 > 5000.0 nM -