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CHEMBL258221 (CID 24868215) - Compound BioActivity Data
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BioActivity Outcomes:
Active(3)
 
 
Inactive(29)
 
 
Inconclusive(1)
 
 
Unspecified(2)
 
 
Top Targets:
NR LBD ROR li..(2)
 
 
SLT beta(2)
 
 
HELICc(2)
 
 
Bromo ALL-1(2)
 
 
Menin(2)
 
 
BioAssay Types:
Confirmatory(25)
 
 
 
Screening(5)
 
 
Literature(5)
 
 
 
BioActivity Types:
Potency(25)
 
 
 
Ki(3)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 31    Data Row: 35   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103561932]
Ki 0.0026Displacement of [3H]neurotensin from pig NTR1 [AID314664, Type: Literature]
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2
[SID103561932]
Ki 0.0027Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells [AID593495, Type: Literature]Neurotensin receptor type 1 [gi:62297312]
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3
[SID103561932]
Ki 0.0061Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells [AID593496, Type: Literature]Neurotensin receptor type 2 [gi:311033404]
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4
[SID103561932]
Agonist activity at NTR1 assessed as effect on intracellular calcium accumulation relative to neurotensin by cell based assay [AID314665, Type: Literature]
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5
[SID103561932]
Selectivity ratio of Ki for human NTS1 to Ki for human NTS2 [AID593497, Type: Literature]
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6
[SID50112527]
Potency 26.6795qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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7
[SID50112527]
Potency qHTS Assay for Inhibitors of Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) [AID1490, Type: confirmatory]phosphopantetheinyl transferase [Bacillus subtilis] [gi:10954339]
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8
[SID50112527]
Potency qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Fluorescein Labeled MLL-derived Peptide [AID1766, Type: confirmatory]menin isoform 1 [Homo sapiens] [gi:18860839]
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9
[SID50112527]
Potency qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Texas Red Labeled MLL-derived Mutant Peptide [AID1768, Type: confirmatory]menin isoform 1 [Homo sapiens] [gi:18860839]
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10
[SID50112527]
Potency qHTS Assay for Inhibitors of Tyrosyl-DNA Phosphodiesterase (TDP1) [AID485290, Type: confirmatory]Chain A, Crystal Structure Of Human Tyrosyl-Dna Phosphodiesterase (Tdp1) [gi:20150581]
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11
[SID50112527]
A qHTS for Small Molecule Inhibitors of Shiga Toxin [AID2315, Type: screening]shiga toxin 1 variant A subunit [Escherichia coli O157:H7] [gi:32400299]
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12
[SID50112527]
Cycloheximide Counterscreen for Small Molecule Inhibitors of Shiga Toxin [AID2314, Type: screening]shiga toxin 1 variant A subunit [Escherichia coli O157:H7] [gi:32400299]
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13
[SID50112527]
Cycloheximide Counterscreen for Small Molecule Inhibitors of Shiga Toxin [AID2314, Type: screening]shiga toxin 1 B subunit [Escherichia coli O157:H7] [gi:32400300]
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14
[SID50112527]
A qHTS for Small Molecule Inhibitors of Shiga Toxin [AID2315, Type: screening]shiga toxin 1 B subunit [Escherichia coli O157:H7] [gi:32400300]
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15
[SID50112527]
Potency qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Fluorescein Labeled MLL-derived Peptide [AID1766, Type: confirmatory]histone-lysine N-methyltransferase 2A isoform 2 precursor [Homo sapiens] [gi:56550039]
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16
[SID50112527]
Potency qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Texas Red Labeled MLL-derived Mutant Peptide [AID1768, Type: confirmatory]histone-lysine N-methyltransferase 2A isoform 2 precursor [Homo sapiens] [gi:56550039]
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17
[SID50112527]
Potency qHTS for Inhibitors of binding or entry into cells for Lassa Virus [AID720533, Type: confirmatory]
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18
[SID50112527]
Potency qHTS for Inhibitors of binding or entry into cells for Marburg Virus [AID720532, Type: confirmatory]gene 4 small orf - Marburg virus [gi:420597]
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19
[SID50112527]
Potency qHTS Assay for Inhibitors and Activators of N370S glucocerebrosidase as a Potential Chaperone Treatment of Gaucher Disease [AID2101, Type: confirmatory]glucocerebrosidase [Homo sapiens] [gi:496369]
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20
[SID50112527]
Potency qHTS Assay for Inhibitors and Activators of Human alpha-Galactosidase From Spleen Homogenate [AID2107, Type: confirmatory]alpha-galactosidase [Homo sapiens] [gi:757912]
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21
[SID50112527]
Potency qHTS Assay for Inhibitors of Bloom's syndrome helicase (BLM) [AID2528, Type: confirmatory]Bloom syndrome protein isoform 1 [Homo sapiens] [gi:4557365]
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22
[SID50112527]
Potency qHTS Assay for Compounds Blocking the Interaction Between CBF-beta and RUNX1 for the Treatment of Acute Myeloid Leukemia [AID1477, Type: confirmatory]
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23
[SID50112527]
qHTS Assay for Inhibitors of Fructose-1,6-bisphosphate Aldolase from Giardia Lamblia: Coupling assay counterscreen [AID2472, Type: screening]glyceraldehyde-3-phosphate dehydrogenase isoform 1 [Homo sapiens] [gi:7669492]
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24
[SID50112527]
Potency Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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25
[SID50112527]
Potency qHTS Assay for Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate [AID2112, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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26
[SID50112527]
Potency qHTS Assay for Inhibitors of Fructose-1,6-bisphosphate Aldolase from Giardia Lamblia [AID2451, Type: confirmatory]Chain A, Structure Of Giardia Fructose-1,6-biphosphate Aldolase In Complex With Phosphoglycolohydroxamate [gi:122920737]
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27
[SID50112527]
Potency qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
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28
[SID50112527]
Potency qHTS for Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in Human Glioma: qHTS [AID602332, Type: confirmatory]heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) [Homo sapiens] [gi:168984549]
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29
[SID50112527]
Potency qHTS for inhibitors of ROR gamma transcriptional activity [AID2551, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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30
[SID50112527]
Potency VP16 counterscreen qHTS for inhibitors of ROR gamma transcriptional activity [AID2546, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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31
[SID50112527]
Potency qHTS for Inhibitors of the Interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2 [AID1469, Type: confirmatory]thyroid hormone receptor beta [Homo sapiens] [gi:189491771]
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32
[SID50112527]
Potency Total Fluorescence Counterscreen for Inhibitors of the Interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2 [AID1479, Type: confirmatory]thyroid hormone receptor beta [Homo sapiens] [gi:189491771]
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33
[SID50112527]
Potency qHTS Assay for Identification of Novel General Anesthetics [AID485281, Type: confirmatory]Chain A, Horse Spleen Apoferritin [gi:254220970]
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34
[SID50112527]
Potency qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) [AID2549, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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35
[SID50112527]
Potency 0.3162qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) [AID2517, Type: confirmatory]Chain A, Human Ape1 Endonuclease With Bound Abasic Dna And Mn2+ Ion [gi:6980812]
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