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Assay Detail

CHEMBL1007257

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Functional
Agonist activity at VDR assessed as receptor transactivation by transient transcription assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Vitamin D3 receptor (CHEMBL1977)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Crystal structures of rat vitamin D receptor bound to adamantyl vitamin D analogs: structural basis for vitamin D receptor antagonism and partial agonism.
Nakabayashi M, Yamada S, Yoshimoto N, Tanaka T, Igarashi M, Ikura T, Ito N, Makishima M, Tokiwa H, DeLuca HF, Shimizu M.
J Med Chem (2008) 51 : 5320 -5329
PubMed 18710208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 9.11 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL467212 1 10.70
CHEMBL466792 1 9.00
CHEMBL452878 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL467212 EC50 = 0.02 nM 10.70
CHEMBL466792 EC50 = 1.0 nM 9.00
CHEMBL452878 EC50 = 24.0 nM 7.62