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US-2015369800-A1 · Dec 24, 2015 · US
Methods for measuring small molecule affinity to cereblon
US2021102938A1 · US · A1
| Field | Value |
|---|---|
| Publication number | US-2021102938-A1 |
| Application number | US-202017026105-A |
| Country | US |
| Kind code | A1 |
| Filing date | Sep 18, 2020 |
| Priority date | Feb 3, 2017 |
| Publication date | Apr 8, 2021 |
| Grant date | — |
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Abstract
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A complex comprises a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN, and uses thereof for identifying therapeutic compounds.
First claim
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1 . A complex comprising (i) a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and (ii) a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN. 2 . The complex of claim 1 , further comprising a DDB1. 3 . The complex of claim 1 , wherein the Cy5-conjugated small molecule binds in a hydrophobic tri-tryptophan pocket formed by Trp380, Trp386, and Trp400 on the CRBN. 4 . The complex of claim 1 , wherein the Cy5-conjugated small molecule has a structure of Formula (I) 5 - 35 . (canceled) 36 . The complex of claim 2 , wherein the Cy5-conjugated small molecule binds in a hydrophobic tri-tryptophan pocket formed by Trp380, Trp386, and Trp400 on the CRBN. 37 . The complex of claim 2 , wherein the Cy5-conjugated small molecule has a structure of Formula (I) 38 . The complex of claim 2 , wherein the complex is prepared by mixing 6xHis-CRBN-DDB1 complex with europium-anti-his antibody and the Cy5-conjugated small molecule of Formula (I). 39 . The complex of claim 38 , wherein the complex is prepared by mixing 60 nM 6xHis-CRBN-DDB1, 3 nM europium-anti-his antibody, and 30 nM Cy5-conjugated small molecule of Formula (I). 40 . A composition comprising the complex of claim 1 . 41 . A composition comprising the complex of claim 2 .
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Classifications
- G01N33/542Primary
with steric inhibition or signal modification, e.g. fluorescent quenching · CPC title
Regulators; Modulating activity · CPC title
from mammals · CPC title
Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A) · CPC title
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- What does patent US2021102938A1 cover?
- A complex comprises a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN, and uses thereof for identifying therapeutic compounds.
- Who is the assignee on this patent?
- Celgene Corp
- What technology area does this patent fall under?
- Primary CPC classification G01N33/542. Mapped technology areas include Physics.
- When was this patent published?
- Publication date Thu Apr 08 2021 00:00:00 GMT+0000 (Coordinated Universal Time) (A1). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).