Assay Providers: Drs. Jose Luis Millan and Eduard Sergienko, Sanford-Burnham Medical Research Institute, San Diego, CA. ..more
Target
Depositor Specified Assays
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| AID | Name | Type | Comment |
|---|---|---|---|
| 518 | TNAP luminescent HTS assay | confirmatory | TNAP luminescent HTS assay |
| 813 | HTS identification of compounds activating TNAP at intermediate concentration of phosphate acceptor detected in luminescent assay | screening | HTS identification of compounds activating TNAP at intermediate concentration of phosphate acceptor detected in luminescent assay |
| 1001 | uHTS identification of compounds activating TNAP in the absence of phosphate acceptor performed in luminescent assay | confirmatory | uHTS identification of compounds activating TNAP in the absence of phosphate acceptor performed in luminescent assay |
| 1136 | uHTS identification of compounds activating TNAP at a high concentration of phosphate acceptor detected in a luminescent assay | screening | uHTS identification of compounds activating TNAP at a high concentration of phosphate acceptor detected in a luminescent assay |
| 1227 | GAPDH Dose Response Colorimetric Assay | confirmatory | GAPDH Dose Response Colorimetric Assay |
| 1450 | SAR assay for compounds activating TNAP in the absence of phosphate acceptor performed in a luminescent assay | confirmatory | SAR assay for compounds activating TNAP in the absence of phosphate acceptor performed in a luminescent assay |
| 1659 | SAR assay for compounds activating TNAP in the presence of 100 mM DEA performed in a luminescence assay | confirmatory | SAR assay for compounds activating TNAP in the presence of 100 mM DEA performed in a luminescence assay |
| 1056 | SAR analysis of an In Vitro TNAP Dose Response Luminescent Assay | confirmatory | |
| 1941 | SAR assay for compounds inhibiting TNAP in the absence of phosphate acceptor performed in a luminescent assay | confirmatory |
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).
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
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| Score | The BioAssay activity ranking score |  | Integer | |||
| 1 | ML# | ML# of the compound | String |
Additional Information
Grant Number: 1R03 MH082385-01
Data Table (Concise)
Classification
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