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BioAssay: AID 1548

Summary assay for compounds activating TNAP performed in a luminescent assay

Assay Providers: Drs. Jose Luis Millan and Eduard Sergienko, Sanford-Burnham Medical Research Institute, San Diego, CA. ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Probe(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Probe(2)
 
 
Active(2)
 
 
AID: 1548
Data Source: Burnham Center for Chemical Genomics (BCCG-A148-TNAP_Activator_Summary_Assay)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-03-12
Modify Date: 2010-12-30

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: Chemical Probe: 2    Active: 2
Depositor Specified Assays
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AIDNameTypeComment
518TNAP luminescent HTS assayconfirmatoryTNAP luminescent HTS assay
813HTS identification of compounds activating TNAP at intermediate concentration of phosphate acceptor detected in luminescent assayscreeningHTS identification of compounds activating TNAP at intermediate concentration of phosphate acceptor detected in luminescent assay
1001uHTS identification of compounds activating TNAP in the absence of phosphate acceptor performed in luminescent assayconfirmatoryuHTS identification of compounds activating TNAP in the absence of phosphate acceptor performed in luminescent assay
1136uHTS identification of compounds activating TNAP at a high concentration of phosphate acceptor detected in a luminescent assayscreeninguHTS identification of compounds activating TNAP at a high concentration of phosphate acceptor detected in a luminescent assay
1227GAPDH Dose Response Colorimetric AssayconfirmatoryGAPDH Dose Response Colorimetric Assay
1450SAR assay for compounds activating TNAP in the absence of phosphate acceptor performed in a luminescent assayconfirmatorySAR assay for compounds activating TNAP in the absence of phosphate acceptor performed in a luminescent assay
1659SAR assay for compounds activating TNAP in the presence of 100 mM DEA performed in a luminescence assayconfirmatorySAR assay for compounds activating TNAP in the presence of 100 mM DEA performed in a luminescence assay
1056SAR analysis of an In Vitro TNAP Dose Response Luminescent Assayconfirmatory
1941SAR assay for compounds inhibiting TNAP in the absence of phosphate acceptor performed in a luminescent assayconfirmatory
Description:
Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG)
Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA)
Network: NIH Molecular Libraries Screening Centers Network (MLSCN)
Grant Proposal Number: 1R03 MH082385-01
Assay Providers: Drs. Jose Luis Millan and Eduard Sergienko, Sanford-Burnham Medical Research Institute, San Diego, CA.

Alkaline phosphatases (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing phosphate and alcohol. APs are dimeric enzymes found in the most organisms. In human, four isozymes of APs have been identified. Three isozymes are tissue-specific and the fourth one is tissue-non specific, named TNAP. TNAP deficiency is associated with defective bone mineralization in the form of rickets and osteomalacia. Therefore, there is therapeutic potential of modulating TNAP activity.

The goal of this HTS is to identify novel and specific activators of TNAP. The only known to date class of alkaline phosphatases activators are amino-containing alcohols, such as diethanolamine (DEA), that act as phosphoacceptor substrate and exhibit its effect in high-mM concentration range. Compounds with a similar mode of action are expected to demonstrate diminished stimulating potential if tested in the presence of DEA. Therefore, for detection of compounds with diverse mode of action, the HTS assay was optimized and HTS campaigns were performed in the presence and in the absence of DEA. The current AID reports a set of the data from screening in the absence of DEA or any other phosphate acceptor.

AIDs 518, 813, 1001, 1136, 1227, 1450 and 1659 were carried out to select probe molecules SID48410176(ML088) and SID56373763(ML087).
Protocol
Please see pertinent AIDs: 518, 813, 1001, 1136, 1227, 1450, 1659
Comment
This AID is used to summarize the results of this MLPCN project. Probe molecules are defined as the positives of this assay and assigned a score of 100
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1ML#ML# of the compoundString
Additional Information
Grant Number: 1R03 MH082385-01

Data Table (Concise)
Classification
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