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Assay Detail

CHEMBL4417024

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of FITC-labelled DEEEIDVVSVE from N-terminal SUMO-fused 6His-tagged WDR5 (unknown origin) (22 to 334 residues) expressed in Escherichia coli BL21(DE3) shaken for 2 mins and incubated for 60 mins by fluorescence polarization assay
ChEMBL ↗
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

WD repeat-containing protein 5 (CHEMBL1075317) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.
Macdonald JD, Chacón Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW.
J Med Chem (2019) 62 : 11232 -11259
PubMed 31724864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 74 6.43 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446534 — — 1 7.54
CHEMBL4535695 — — 1 7.52
CHEMBL4437642 — — 1 7.51
CHEMBL4483349 — — 1 7.42
CHEMBL4552035 — — 1 7.35
CHEMBL4450684 — — 1 7.34
CHEMBL4468085 — — 1 7.33
CHEMBL4544635 — — 1 7.33
CHEMBL4518895 — — 1 7.30
CHEMBL4529202 — — 1 7.29
CHEMBL4474057 — — 1 7.19
CHEMBL4441676 — — 1 7.17
CHEMBL4472649 — — 1 7.16
CHEMBL4589677 — — 1 7.03
CHEMBL4528788 — — 1 6.98
CHEMBL4569742 — — 1 6.96
CHEMBL4573903 — — 1 6.96
CHEMBL4455527 — — 1 6.91
CHEMBL4578283 — — 1 6.91
CHEMBL4471200 — — 1 6.91
CHEMBL4549544 — — 1 6.89
CHEMBL4575067 — — 1 6.86
CHEMBL4518711 — — 1 6.79
CHEMBL4554506 — — 1 6.78
CHEMBL4473507 — — 1 6.74
CHEMBL4455721 — — 1 6.72
CHEMBL4469816 — — 1 6.71
CHEMBL4471282 — — 1 6.71
CHEMBL4523046 — — 1 6.69
CHEMBL4586914 — — 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446534 — Kd = 29.0 nM 7.54
CHEMBL4535695 — Kd = 30.0 nM 7.52
CHEMBL4437642 — Kd = 31.0 nM 7.51
CHEMBL4483349 — Kd = 38.0 nM 7.42
CHEMBL4552035 — Kd = 45.0 nM 7.35
CHEMBL4450684 — Kd = 46.0 nM 7.34
CHEMBL4468085 — Kd = 47.0 nM 7.33
CHEMBL4544635 — Kd = 47.0 nM 7.33
CHEMBL4518895 — Kd = 50.0 nM 7.30
CHEMBL4529202 — Kd = 51.0 nM 7.29
CHEMBL4474057 — Kd = 64.0 nM 7.19
CHEMBL4441676 — Kd = 67.0 nM 7.17
CHEMBL4472649 — Kd = 69.0 nM 7.16
CHEMBL4589677 — Kd = 93.0 nM 7.03
CHEMBL4528788 — Kd = 104.0 nM 6.98
CHEMBL4569742 — Kd = 110.0 nM 6.96
CHEMBL4573903 — Kd = 110.0 nM 6.96
CHEMBL4455527 — Kd = 123.0 nM 6.91
CHEMBL4578283 — Kd = 122.0 nM 6.91
CHEMBL4471200 — Kd = 122.0 nM 6.91
CHEMBL4549544 — Kd = 128.0 nM 6.89
CHEMBL4575067 — Kd = 137.0 nM 6.86
CHEMBL4518711 — Kd = 163.0 nM 6.79
CHEMBL4554506 — Kd = 167.0 nM 6.78
CHEMBL4473507 — Kd = 184.0 nM 6.74
CHEMBL4455721 — Kd = 190.0 nM 6.72
CHEMBL4471282 — Kd = 195.0 nM 6.71
CHEMBL4469816 — Kd = 194.0 nM 6.71
CHEMBL4523046 — Kd = 204.0 nM 6.69
CHEMBL4586914 — Kd = 207.0 nM 6.68
CHEMBL4447845 — Kd = 215.0 nM 6.67
CHEMBL4534549 — Kd = 220.0 nM 6.66
CHEMBL4573789 — Kd = 223.0 nM 6.65
CHEMBL4537674 — Kd = 229.0 nM 6.64
CHEMBL4473122 — Kd = 229.0 nM 6.64
CHEMBL4594023 — Kd = 238.0 nM 6.62
CHEMBL4476737 — Kd = 272.0 nM 6.57
CHEMBL4470498 — Kd = 289.0 nM 6.54
CHEMBL4535470 — Kd = 298.0 nM 6.53
CHEMBL4532703 — Kd = 304.0 nM 6.52
CHEMBL4465645 — Kd = 349.0 nM 6.46
CHEMBL4441794 — Kd = 362.0 nM 6.44
CHEMBL4458101 — Kd = 385.0 nM 6.42
CHEMBL4515727 — Kd = 431.0 nM 6.37
CHEMBL4475470 — Kd = 511.0 nM 6.29
CHEMBL4583201 — Kd = 547.0 nM 6.26
CHEMBL4462398 — Kd = 549.0 nM 6.26
CHEMBL4543629 — Kd = 566.0 nM 6.25
CHEMBL4434999 — Kd = 614.0 nM 6.21
CHEMBL4553810 — Kd = 746.0 nM 6.13