Date: Tue Jan 7th 2025
Time: 2pm UK time (other times)
Place: Zoom link
Previous Meeting: issue #22
Who can come?: Anyone. No need to say anything unless you'd like to. If you'd like to contribute, please join Github.
Attendees: Dr Eve Carter (UCL), Dr Madison Edwards (Uni Toronto), Prof Matt Todd (UCL), Dr Claudia Tredup (Goethe-University Frankfurt), Anna Girtle (Uni Toronto), Dr Jeffrey Mowat (Janssen Pharmaceutica NV).
Decks: Eve's presentation
Agenda:
In meeting:
Eve presented the results of an ASMS screen performed by the SGC in Toronto with chicken PLCz1 from Madison and PLCg1 from Matilda Katan. All of the hit molecules are small, and should be commercially available. Eve has been able to purchase 12 of the 14 hits, which she will test in the Aldol assay at UCL once they arrive. The two remaining compounds are not commercially available. SGC Toronto will perform SPR analysis on the hit structures. Eve planned to purchase analogues of any compounds that look promising after these additional assays, but Claudia has advised that she should purchase them now as there is a fairly long lead time of several weeks before they could be delivered. Once compounds have been delivered, Eve will ship them to Nuvisan to test in their orthogonal assays.
Eve also presented the results of assays performed by Nuvisan with the four best hits from the SGC DCP library. These structures initially looked promising from results in the Aldol assay using chicken PLCz1. When human PLCz1 (with a contaminant present) was used in an XY-69 assay, FM-743 and SGK3 PROTAC look promising, but the two Bayer molecules have IC50 values of >25 uM. Similar results were observed with PLCd1. No compounds were particularly active in the IP-One and diC8 assays. For now, focus will move away from these results to prioritise the ASMS results.
Madison will prepare stock solutions to send, together with protein samples, to HitGen to perform a DEL screen.
To do:
L'esprit de l'escalier
If you'd like to follow up after the meeting, please comment below. You can also email, but please be clear if anything in the email should not be public domain - the default is open.
Next meeting: 8th April 2025, 2pm UK time
Date: Tue Jan 7th 2025
Time: 2pm UK time (other times)
Place: Zoom link
Previous Meeting: issue #22
Who can come?: Anyone. No need to say anything unless you'd like to. If you'd like to contribute, please join Github.
Attendees: Dr Eve Carter (UCL), Dr Madison Edwards (Uni Toronto), Prof Matt Todd (UCL), Dr Claudia Tredup (Goethe-University Frankfurt), Anna Girtle (Uni Toronto), Dr Jeffrey Mowat (Janssen Pharmaceutica NV).
Decks: Eve's presentation
Agenda:
In meeting:
Eve presented the results of an ASMS screen performed by the SGC in Toronto with chicken PLCz1 from Madison and PLCg1 from Matilda Katan. All of the hit molecules are small, and should be commercially available. Eve has been able to purchase 12 of the 14 hits, which she will test in the Aldol assay at UCL once they arrive. The two remaining compounds are not commercially available. SGC Toronto will perform SPR analysis on the hit structures. Eve planned to purchase analogues of any compounds that look promising after these additional assays, but Claudia has advised that she should purchase them now as there is a fairly long lead time of several weeks before they could be delivered. Once compounds have been delivered, Eve will ship them to Nuvisan to test in their orthogonal assays.
Eve also presented the results of assays performed by Nuvisan with the four best hits from the SGC DCP library. These structures initially looked promising from results in the Aldol assay using chicken PLCz1. When human PLCz1 (with a contaminant present) was used in an XY-69 assay, FM-743 and SGK3 PROTAC look promising, but the two Bayer molecules have IC50 values of >25 uM. Similar results were observed with PLCd1. No compounds were particularly active in the IP-One and diC8 assays. For now, focus will move away from these results to prioritise the ASMS results.
Madison will prepare stock solutions to send, together with protein samples, to HitGen to perform a DEL screen.
To do:
L'esprit de l'escalier
If you'd like to follow up after the meeting, please comment below. You can also email, but please be clear if anything in the email should not be public domain - the default is open.
Next meeting: 8th April 2025, 2pm UK time