Versioned source-reviewed overlay · Phase 6B
Experimental Bioactivity
Primary-source observations, original endpoints, explicit target/construct scope and documented gaps. Phase 5 and Phase 6A remain frozen.
4 matching observations · 3 preparations
Phase 6B additions only; Phase 6A's baseline 80 remain separately accessible.
| Preparation | Target and scope | Method and original endpoint | Source and verification | Structure / limitations |
|---|---|---|---|---|
| UNC10088published name only exact assayed identity unresolved | NSD2 PWWP1 — exact domainHis-tagged NSD2 PWWP1; exact sequence boundaries not independently extracted | TR-FRET competitive displacement of biotinylated UNC7096 IC50 =248 ± 22 nMSEM · n=3 independent experiments | 10.1038/s41467-026-72235-9Figure 2h and Supplementary Figure 3Daccepted with bounded interpretation | Transformed compound in ternary complex — not unmodified parent binaryInterpretation and limitationspositive competitive engagement; not an equilibrium Kd The prepared chemical parent is not stereochemistry/batch resolved; IC50 not Kd. Do not count FBXO22-conditional results as independent chemical identities. Without FBXO22 FIST domain |
| UNC10088published name only exact assayed identity unresolved | NSD2 PWWP1 — exact domainHis-tagged NSD2 PWWP1 + FBXO22 FIST; exact sequence boundaries not independently extracted | TR-FRET competitive displacement of biotinylated UNC7096 IC50 =101 ± 8 nMSEM · n=3 independent experiments | 10.1038/s41467-026-72235-9Figure 2h, Supplementary Figure 3D and Resultsaccepted with bounded interpretation | Transformed compound in ternary complex — not unmodified parent binaryInterpretation and limitationspositive cooperative engagement in a ternary context; not an equilibrium Kd Two different experimental contexts for one preparation; do not average or replace one with another. With wild-type FBXO22 FIST domain; source-reported cooperative factor alpha = 3.3, not 248/101 |
| UNC10415667published name only exact assayed identity unresolved | NSD2 — cellular, whole proteinU2OS NSD2-HiBiT cells | Cellular HiBiT protein-degradation dose response DC50 =460 nMfigure caption reports SEM but numeric uncertainty was not independently extracted · n=2 independent experiments (final 2026 article) | 10.1038/s41467-026-72235-9Figure 3e legend and Resultsaccepted with bounded interpretation | Transformed compound in ternary complex — not unmodified parent binaryInterpretation and limitationscellular whole-protein depletion; no isolated-domain affinity Do not copy this whole-protein DC50 to NSD2 PWWP1. 75% at 1 µM for 6 hours is a separate endpoint, not the same dose-response value. U2OS NSD2 HiBiT dose response |
| UNC12149published name only exact assayed identity unresolved | NSD2 — cellular, whole proteinU2OS NSD2-HiBiT cells | Cellular HiBiT protein-degradation dose response DC50 =120 nMfigure caption reports SEM but numeric uncertainty was not independently extracted · n=2 independent experiments (final 2026 article) | 10.1038/s41467-026-72235-9Figure 4h legend and Resultsaccepted with bounded interpretation | No verified PWWP-bound experimental binary structureInterpretation and limitationscellular whole-protein depletion; no isolated-domain affinity Do not transfer cellular DC50 to a particular PWWP-domain biochemical binding constant. U2OS NSD2 HiBiT dose response |
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