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Assay Detail

CHEMBL1641107

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

Functional
Induction of differentiation of human HL60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HL-60
Confidence 1 — Organism
Curated By Autocuration

Target

HL-60 (CHEMBL383)
Type CELL-LINE
Organism Homo sapiens

Publication

Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.
Grzywacz P, Chiellini G, Plum LA, Clagett-Dame M, DeLuca HF.
J Med Chem (2010) 53 : 8642 -8649
PubMed 21105677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.74 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL605525 DP001 2.0 1 10.10
CHEMBL1630755 1 10.05
CHEMBL1630759 1 10.00
CHEMBL1630757 1 9.40
CHEMBL3085140 1 9.22
CHEMBL1630754 1 9.00
CHEMBL846 CALCITRIOL 4.0 1 8.70
CHEMBL3085139 1 8.70
CHEMBL1630758 1 8.70
CHEMBL1630756 1 8.30
CHEMBL1630763 1 8.22
CHEMBL1630761 1 7.70
CHEMBL1630762 1 7.22
CHEMBL1630760 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL605525 DP001 Ki = 0.08 nM 10.10
CHEMBL1630755 Ki = 0.09 nM 10.05
CHEMBL1630759 Ki = 0.1 nM 10.00
CHEMBL1630757 Ki = 0.4 nM 9.40
CHEMBL3085140 Ki = 0.6 nM 9.22
CHEMBL1630754 Ki = 1.0 nM 9.00
CHEMBL846 CALCITRIOL Ki = 2.0 nM 8.70
CHEMBL3085139 Ki = 2.0 nM 8.70
CHEMBL1630758 Ki = 2.0 nM 8.70
CHEMBL1630756 Ki = 5.0 nM 8.30
CHEMBL1630763 Ki = 6.0 nM 8.22
CHEMBL1630761 Ki = 20.0 nM 7.70
CHEMBL1630762 Ki = 60.0 nM 7.22
CHEMBL1630760 Ki = 100.0 nM 7.00