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BioAssay: AID 1577

Summary luminescent assay for discovery of chemical inhibitors of placental alkaline phosphatase

Alkaline phosphatase (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing phosphate and alcohol. APs are dimeric enzymes found in most organisms. In human, four isozymes of APs have been identified: three isozymes are tissue-specific and the fourth one is tissue-nonspecific. Placental alkaline phosphatase (PLAP) is highly expressed in primate placental tissue. Its biological function is unknown. Identification of PLAP-specific inhibitors should provide necessary tools for characterization of its biological role. ..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: 1577
Data Source: Burnham Center for Chemical Genomics (BCCG-A160-PLAP-Summary-Assay)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-03-23
Modify Date: 2010-12-30

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: Chemical Probe: 2    Active: 2
Related Experiments
AIDNameTypeComment
518TNAP luminescent HTS assayConfirmatorydepositor-specified cross reference: TNAP luminescent HTS assay
690Luminescent assay for HTS discovery of chemical inhibitors of placental alkaline phosphataseConfirmatorydepositor-specified cross reference: Luminescent assay for HTS discovery of chemical inhibitors of placental alkaline phosphatase
696Luminescent assay for HTS discovery of chemical activators of placental alkaline phosphataseConfirmatorydepositor-specified cross reference: Luminescent assay for HTS discovery of chemical activators of placental alkaline phosphatase
1017Luminescent assay for identification of inhibitors of human intestinal alkaline phosphataseConfirmatorydepositor-specified cross reference: Luminescent assay for identification of inhibitors of human intestinal alkaline phosphatase
1019Luminescent assay for identification of inhibitors of bovine intestinal alkaline phosphataseScreeningdepositor-specified cross reference: Luminescent assay for identification of inhibitors of bovine intestinal alkaline phosphatase
1056SAR analysis of an In Vitro TNAP Dose Response Luminescent AssayConfirmatorydepositor-specified cross reference: In Vitro TNAP Dose Response Luminescent Assay for SAR Study
1512Luminescent assay for HTS discovery of chemical inhibitors of placental alkaline phosphatase confirmationConfirmatorydepositor-specified cross reference: Luminescent assay for HTS discovery of chemical inhibitors of placental alkaline phosphatase confirm
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: MH077602-01
Assay Provider: Dr. Jose Luis Millan, Sanford-Burnham Medical Research Institute, San Diego, CA.

Alkaline phosphatase (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing phosphate and alcohol. APs are dimeric enzymes found in most organisms. In human, four isozymes of APs have been identified: three isozymes are tissue-specific and the fourth one is tissue-nonspecific. Placental alkaline phosphatase (PLAP) is highly expressed in primate placental tissue. Its biological function is unknown. Identification of PLAP-specific inhibitors should provide necessary tools for characterization of its biological role.

PLAP screening was developed and performed at the Sanford-Burnham Center for Chemical Genomics (SBCCG) as part of the Molecular Library Screening Center Network (MLSCN). AID 690 was a selectivity screening for tissue nonspecific alkaline phosphatase (TNAP) screened at SBCCG (AID 518). XO1 submission, MH077602-01, Pharmacological inhibitors of tissue-nonspecific alkaline phosphatase (TNAP), Assay Provider Dr. Jose Luis Millan, Sanford-Burnham Medical Research Institute, San Diego, CA.

AIDs 518, 690, 696, 1017, 1019 and 1512 were carried out to select probe molecules SID-56373725(ML085) and SID-56405584(ML095).
Protocol
Please see pertinent AIDs: 518, 690, 696, 1017, 1019, 1056, 1512
Comment
Probe molecules are defined as the positives of this assay and assigned a score of 100
Categorized Comment - additional comments and annotations
From MLP Probe Report:
Probe count: 2
MLP Probe ML# for probe 1: ML085
PubChem Substance ID (SID) for probe 1: 56373725
PubChem Compound ID (CID) for probe 1: 665093
Probe type for probe 1: Inhibitor
IC50/EC50 (nM) for probe 1: 2600
Target for probe 1: PLAP (gi: 157266296)
Anti-target for probe 1: TNAP
Fold selectivity for probe 1: >42
NCBI Book chapter link for probe 1: http://www.ncbi.nlm.nih.gov/books/NBK47343/ (ID: 2358778)
Grant number for probe 1: MH077602-01
MLP Probe ML# for probe 2: ML095
PubChem Substance ID (SID) for probe 2: 56405584
PubChem Compound ID (CID) for probe 2: 25067483
Probe type for probe 2: Inhibitor
IC50/EC50 (nM) for probe 2: 4240
Target for probe 2: PLAP (gi: 157266296)
Anti-target for probe 2: TNAP
Fold selectivity for probe 2: >27
NCBI Book chapter link for probe 2: http://www.ncbi.nlm.nih.gov/books/NBK47351/ (ID: 2359532)
Grant number for probe 2: MH077602-01
NCBI Book chapter title for probe 1: Placental Alkaline Phosphatase (PLAP) Luminescent HTS assay - Probe 1
NCBI Book chapter title for probe 2: Placental Alkaline Phosphatase (PLAP) Luminescent HTS assay - Probe 2
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1ML#ML# for the compoundString
Additional Information
Grant Number: MH081277-01

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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