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Assay Detail

CHEMBL937973

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

Functional
Antiproliferative activity against human HL60 cells assessed as inhibition of [3H]thymidine incorporation after 4 days by liquid scintillation counter
33
Total Activities
33
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

Novel esters of glaucarubolone as inducers of terminal differentiation of promyelocytic HL-60 cells and inhibitors of 7,12-dimethylbenz[a]anthracene-induced preneoplastic lesion formation in mouse mammary organ culture.
Mata-Greenwood E, Daeuble JF, Grieco PA, Dou J, McChesney JD, Mehta RG, Kinghorn AD, Pezzuto JM.
J Nat Prod (2001) 64 : 1509 -1513
PubMed 11754601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.70 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444949 1 8.05
CHEMBL452138 1 8.05
CHEMBL500033 1 7.96
CHEMBL509895 BRUCEANTIN 1 7.40
CHEMBL509858 1 7.40
CHEMBL463295 1 7.40
CHEMBL444177 QUASSIMARIN 1 7.22
CHEMBL450464 BRUSATOL 1 7.16
CHEMBL504648 1 7.16
CHEMBL506841 1 7.12
CHEMBL486998 SOULARUBINONE 1 7.00
CHEMBL448765 1 6.82
CHEMBL501007 1 6.72
CHEMBL494560 1 6.70
CHEMBL498937 1 6.70
CHEMBL519243 HOLACANTHONE 1 6.70
CHEMBL494374 1 6.58
CHEMBL521129 SAMADERIN B 1 6.40
CHEMBL507027 1 6.40
CHEMBL523681 GLAUCARUBOLONE 1 6.40
CHEMBL1202062 1 6.30
CHEMBL458347 GLAUCARUBINONE 1 6.30
CHEMBL493225 1 6.30
CHEMBL487903 1 6.22
CHEMBL446308 1 6.16
CHEMBL487286 1 6.00
CHEMBL487698 1 6.00
CHEMBL472016 CHAPARRINONE 1 5.92
CHEMBL520562 1 5.82
CHEMBL469501 YADANZIOLIDE C 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444949 IC50 = 9.0 nM 8.05
CHEMBL452138 IC50 = 9.0 nM 8.05
CHEMBL500033 IC50 = 11.0 nM 7.96
CHEMBL509895 BRUCEANTIN IC50 = 40.0 nM 7.40
CHEMBL509858 IC50 = 40.0 nM 7.40
CHEMBL463295 IC50 = 40.0 nM 7.40
CHEMBL444177 QUASSIMARIN IC50 = 60.0 nM 7.22
CHEMBL450464 BRUSATOL IC50 = 70.0 nM 7.16
CHEMBL504648 IC50 = 70.0 nM 7.16
CHEMBL506841 IC50 = 75.0 nM 7.12
CHEMBL486998 SOULARUBINONE IC50 = 100.0 nM 7.00
CHEMBL448765 IC50 = 150.0 nM 6.82
CHEMBL501007 IC50 = 190.0 nM 6.72
CHEMBL519243 HOLACANTHONE IC50 = 200.0 nM 6.70
CHEMBL498937 IC50 = 200.0 nM 6.70
CHEMBL494560 IC50 = 200.0 nM 6.70
CHEMBL494374 IC50 = 260.0 nM 6.58
CHEMBL521129 SAMADERIN B IC50 = 400.0 nM 6.40
CHEMBL507027 IC50 = 400.0 nM 6.40
CHEMBL523681 GLAUCARUBOLONE IC50 = 400.0 nM 6.40
CHEMBL1202062 IC50 = 500.0 nM 6.30
CHEMBL458347 GLAUCARUBINONE IC50 = 500.0 nM 6.30
CHEMBL493225 IC50 = 500.0 nM 6.30
CHEMBL487903 IC50 = 600.0 nM 6.22
CHEMBL446308 IC50 = 700.0 nM 6.16
CHEMBL487286 IC50 = 1000.0 nM 6.00
CHEMBL487698 IC50 = 1000.0 nM 6.00
CHEMBL472016 CHAPARRINONE IC50 = 1200.0 nM 5.92
CHEMBL520562 IC50 = 1500.0 nM 5.82
CHEMBL469501 YADANZIOLIDE C IC50 = 1500.0 nM 5.82
CHEMBL488725 IC50 = 3200.0 nM 5.50
CHEMBL480882 SIMALIKALACTONE D IC50 > 200.0 nM -
CHEMBL482808 IC50 > 3000.0 nM -