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Assay Detail

CHEMBL910037

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

Functional
Antagonist activity against 1-alpha,25-dihydroxy vitamin D3-induced HL60 cell differentiation by NBT reduction method
84
Total Activities
84
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HL-60
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones.
Saito N, Matsunaga T, Saito H, Anzai M, Takenouchi K, Miura D, Namekawa J, Ishizuka S, Kittaka A.
J Med Chem (2006) 49 : 7063 -7075
PubMed 17125259 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 84 8.12 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL383910 1 8.22
CHEMBL216037 1 8.22
CHEMBL386412 1 8.22
CHEMBL213868 1 8.22
CHEMBL387098 1 8.22
CHEMBL384614 1 8.22
CHEMBL383850 1 8.22
CHEMBL217385 1 8.21
CHEMBL387220 1 8.21
CHEMBL385205 1 8.21
CHEMBL385705 1 8.21
CHEMBL217924 1 8.21
CHEMBL215164 1 8.21
CHEMBL385707 1 8.21
CHEMBL214978 1 8.21
CHEMBL215239 1 8.20
CHEMBL215360 1 8.20
CHEMBL387281 1 8.20
CHEMBL385342 1 8.20
CHEMBL214500 1 8.20
CHEMBL217417 1 8.20
CHEMBL384370 1 8.20
CHEMBL218565 1 8.20
CHEMBL217447 1 8.20
CHEMBL215306 1 8.20
CHEMBL383902 1 8.20
CHEMBL384929 1 8.20
CHEMBL385926 1 8.20
CHEMBL384020 1 8.17
CHEMBL217030 1 8.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL383910 IC50 = 6.0 nM 8.22
CHEMBL216037 IC50 = 6.0 nM 8.22
CHEMBL386412 IC50 = 6.0 nM 8.22
CHEMBL213868 IC50 = 6.0 nM 8.22
CHEMBL387098 IC50 = 6.0 nM 8.22
CHEMBL384614 IC50 = 6.0 nM 8.22
CHEMBL383850 IC50 = 6.0 nM 8.22
CHEMBL217924 IC50 = 6.1 nM 8.21
CHEMBL387220 IC50 = 6.1 nM 8.21
CHEMBL385205 IC50 = 6.1 nM 8.21
CHEMBL385705 IC50 = 6.1 nM 8.21
CHEMBL217385 IC50 = 6.2 nM 8.21
CHEMBL215164 IC50 = 6.2 nM 8.21
CHEMBL385707 IC50 = 6.2 nM 8.21
CHEMBL214978 IC50 = 6.2 nM 8.21
CHEMBL385342 IC50 = 6.3 nM 8.20
CHEMBL215360 IC50 = 6.3 nM 8.20
CHEMBL387281 IC50 = 6.3 nM 8.20
CHEMBL214500 IC50 = 6.3 nM 8.20
CHEMBL217417 IC50 = 6.3 nM 8.20
CHEMBL384370 IC50 = 6.3 nM 8.20
CHEMBL217447 IC50 = 6.3 nM 8.20
CHEMBL215306 IC50 = 6.3 nM 8.20
CHEMBL383902 IC50 = 6.3 nM 8.20
CHEMBL384929 IC50 = 6.3 nM 8.20
CHEMBL385926 IC50 = 6.3 nM 8.20
CHEMBL215239 IC50 = 6.3 nM 8.20
CHEMBL218565 IC50 = 6.3 nM 8.20
CHEMBL217335 IC50 = 6.7 nM 8.17
CHEMBL386623 IC50 = 6.7 nM 8.17
CHEMBL215968 IC50 = 6.7 nM 8.17
CHEMBL215518 IC50 = 6.7 nM 8.17
CHEMBL215806 IC50 = 6.8 nM 8.17
CHEMBL215173 IC50 = 6.7 nM 8.17
CHEMBL214469 IC50 = 6.7 nM 8.17
CHEMBL217030 IC50 = 6.7 nM 8.17
CHEMBL384020 IC50 = 6.8 nM 8.17
CHEMBL384538 IC50 = 6.7 nM 8.17
CHEMBL214662 IC50 = 7.7 nM 8.11
CHEMBL410320 IC50 = 7.7 nM 8.11
CHEMBL217265 IC50 = 8.2 nM 8.09
CHEMBL213915 IC50 = 8.1 nM 8.09
CHEMBL387286 IC50 = 8.2 nM 8.09
CHEMBL214135 IC50 = 8.1 nM 8.09
CHEMBL214786 IC50 = 8.2 nM 8.09
CHEMBL383856 IC50 = 8.2 nM 8.09
CHEMBL385830 IC50 = 8.4 nM 8.08
CHEMBL214134 IC50 = 8.4 nM 8.08
CHEMBL218183 IC50 = 8.4 nM 8.08
CHEMBL385871 IC50 = 8.4 nM 8.08