Table I. Candidate E-3810 targets identified by the chemoproteomic competition assay. Proteins are grouped in three categories: protein kinases, proteins involved in nicotinamide/nicotinate catalysis, and other proteins. Each protein has an associated p value, used to evaluate the ratio trend from sample A to sample D as either linear (slope test) or logarithmic (plateau). Proteins also found to be putative E-3810 targets in the Kd assay (Table II) are marked with “+”.
| Gene name | UniProt I.D. | Protein name | Slope test | Simple p value | Plateau test | Plateau p value | Present in Table II |
|---|---|---|---|---|---|---|---|
| Protein kinases | |||||||
| PDGFRA | P16234–1 | Platelet-derived growth factor receptor α | −0.26 | 2.5E-02 | −0.86 | 6.8E-05 | + |
| CARDIAK | O43353–1 | Receptor-interacting serine/threonine-protein kinase 2 | −0.24 | 3.3E-02 | −0.82 | 1.9E-05 | + |
| DDR2 | Q16832 | Discoidin domain-containing receptor 2 | −0.27 | 1.6E-02 | −0.86 | 1.3E-07 | + |
| LYNa | Q6NUK7 | LYN protein | −0.31 | 2.9E-03 | −0.86 | 1.3E-04 | + |
| CSBP (1)a | Q16539–2 | Cytokine suppressive anti-inflammatory drug-binding protein | −0.39 | 8.9E-03 | −0.51 | 1.2E-01 | |
| YES | P07947 | Tyrosine protein kinase Yes | −0.28 | 5.9E-06 | −0.53 | 4.5E-02 | + |
| SRC | P12931–2 | Proto-oncogene tyrosine-protein kinase Src | −0.30 | 2.1E-06 | −0.55 | 4.8E-02 | |
| EPHA2 | P29317 | Ephrin type-A receptor 2 | −0.26 | 2.6E-04 | −0.43 | 1.1E-01 | |
| CSNK1E | B3KRV2 | Casein kinase I isoform ϵ | −0.28 | 1.1E-03 | −0.65 | 7.9E-03 | |
| MAP4K4 | O95819–3 | HPK/GCK-like kinase HGK | −0.20 | 9.5E-03 | −0.35 | 1.4E-01 | |
| CSBP (2) | Q16539–1 | Cytokine suppressive anti-inflammatory drug-binding protein | −0.33 | 3.8E-06 | −0.71 | 1.1E-02 | + |
| Nicotinamide/nicotinate catalysis | |||||||
| NMOR2 | P16083 | NAD(P)H dehydrogenase [quinone] 2 | −0.28 | 6.5E-05 | −0.46 | 1.1E-01 | + |
| NMOR1 | P15559 | NAD(P)H dehydrogenase [quinone] 1 | −0.38 | 2.1E-04 | −0.65 | 9.2E-02 | + |
| QPRT | Q15274 | Nicotinate-nucleotide pyrophosphorylase [carboxylating] | −0.21 | 4.0E-02 | −0.20 | 5.1E-01 | + |
| Other proteins | |||||||
| GBAS | O75323 | Protein NipSnap homolog 2 | −0.28 | 8.5E-04 | −0.47 | 1.2E-01 | |
| NIPSNAP1 | Q9BPW8 | Protein NipSnap homolog 1 | −0.30 | 2.3E-04 | −0.46 | 1.5E-01 | + |
| RIE2 | B3KWY9 | Highly similar to RING finger protein 10 | −0.14 | 2.1E-02 | −0.32 | 7.5E-02 | |
| MTIF2 | P46199 | Translation initiation factor IF-2, mitochondrial | −0.17 | 2.2E-02 | −0.15 | 5.0E-01 | |
| RABGGTA | Q92696 | Geranylgeranyl transferase type II subunit α | −0.15 | 8.1E-03 | −0.21 | 2.6E-01 | |
| UBF | P17480–1 | Nucleolar transcription factor 1 | −0.10 | 4.1E-02 | −0.08 | 6.2E-01 | |
| KIAA0197 | Q12769–1 | 160 kDa nucleoporin | −0.15 | 2.1E-03 | −0.20 | 2.3E-01 | |
| TRDX | P10599 | Thioredoxin | −0.10 | 2.9E-05 | −0.19 | 3.5E-02 | + |
a Fragmentation spectra for proteins identified based on two peptides, of which one unique peptide is reported in supplemental Fig. S10.