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Assay Detail

CHEMBL5337544

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

Binding
Inhibition of BRD4 (unknown origin) using BET peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by HTRF assay
ChEMBL ↗
52
Total Activities
52
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

Bromodomain-containing protein 4 (CHEMBL1163125) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Liu J, Huang J, Wang K, Li Y, Li C, Zhu Y, He X, Zhang Y, Zhao Y, Hu C, Xi Z, Tong M, Li Z, Gong P, Hou Y.
Bioorg Med Chem (2024) 101 : 117609 -117609
PubMed 38364599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.55 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5418129 — — 1 7.25
CHEMBL5429440 — — 1 7.22
CHEMBL5419367 — — 1 7.21
CHEMBL1957266 — — 1 7.16
CHEMBL5416208 — — 1 7.15
CHEMBL5422122 — — 1 7.15
CHEMBL513909 BI-2536 2.0 1 7.13
CHEMBL5421238 — — 1 7.12
CHEMBL5401381 — — 1 7.05
CHEMBL5440739 — — 1 7.01
CHEMBL5410968 — — 1 6.95
CHEMBL5426964 — — 1 6.94
CHEMBL1233528 VOLASERTIB 3.0 1 6.92
CHEMBL5438409 — — 1 6.89
CHEMBL5415794 — — 1 6.86
CHEMBL5409453 — — 1 6.81
CHEMBL5403358 — — 1 6.81
CHEMBL5417495 — — 1 6.78
CHEMBL5437669 — — 1 6.74
CHEMBL5394764 — — 1 6.72
CHEMBL5427957 — — 1 6.70
CHEMBL5400502 — — 1 6.67
CHEMBL5402922 — — 1 6.66
CHEMBL5412127 — — 1 6.66
CHEMBL5428087 — — 1 6.66
CHEMBL5403473 — — 1 6.61
CHEMBL5398977 — — 1 6.60
CHEMBL5409700 — — 1 6.54
CHEMBL5406467 — — 1 6.53
CHEMBL5395480 — — 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5418129 — IC50 = 56.7 nM 7.25
CHEMBL5429440 — IC50 = 60.8 nM 7.22
CHEMBL5419367 — IC50 = 61.79 nM 7.21
CHEMBL1957266 — IC50 = 68.9 nM 7.16
CHEMBL5416208 — IC50 = 70.6 nM 7.15
CHEMBL5422122 — IC50 = 70.1 nM 7.15
CHEMBL513909 BI-2536 IC50 = 73.3 nM 7.13
CHEMBL5421238 — IC50 = 75.3 nM 7.12
CHEMBL5401381 — IC50 = 88.6 nM 7.05
CHEMBL5440739 — IC50 = 97.3 nM 7.01
CHEMBL5410968 — IC50 = 112.4 nM 6.95
CHEMBL5426964 — IC50 = 115.8 nM 6.94
CHEMBL1233528 VOLASERTIB IC50 = 119.8 nM 6.92
CHEMBL5438409 — IC50 = 128.1 nM 6.89
CHEMBL5415794 — IC50 = 138.0 nM 6.86
CHEMBL5409453 — IC50 = 155.4 nM 6.81
CHEMBL5403358 — IC50 = 154.6 nM 6.81
CHEMBL5417495 — IC50 = 164.8 nM 6.78
CHEMBL5437669 — IC50 = 181.1 nM 6.74
CHEMBL5394764 — IC50 = 189.9 nM 6.72
CHEMBL5427957 — IC50 = 200.2 nM 6.70
CHEMBL5400502 — IC50 = 211.5 nM 6.67
CHEMBL5402922 — IC50 = 217.6 nM 6.66
CHEMBL5412127 — IC50 = 217.1 nM 6.66
CHEMBL5428087 — IC50 = 218.4 nM 6.66
CHEMBL5403473 — IC50 = 244.2 nM 6.61
CHEMBL5398977 — IC50 = 252.1 nM 6.60
CHEMBL5409700 — IC50 = 289.8 nM 6.54
CHEMBL5406467 — IC50 = 294.4 nM 6.53
CHEMBL5395480 — IC50 = 292.7 nM 6.53
CHEMBL5402431 — IC50 = 300.7 nM 6.52
CHEMBL5437723 — IC50 = 328.1 nM 6.48
CHEMBL5408013 — IC50 = 417.8 nM 6.38
CHEMBL5415796 — IC50 = 522.6 nM 6.28
CHEMBL5421723 — IC50 = 540.4 nM 6.27
CHEMBL5434467 — IC50 = 549.0 nM 6.26
CHEMBL5426693 — IC50 = 572.3 nM 6.24
CHEMBL5408776 — IC50 = 580.3 nM 6.24
CHEMBL5430428 — IC50 = 657.7 nM 6.18
CHEMBL5437467 — IC50 = 790.7 nM 6.10
CHEMBL5412529 — IC50 = 813.7 nM 6.09
CHEMBL5417441 — IC50 = 818.3 nM 6.09
CHEMBL5408583 — IC50 = 856.1 nM 6.07
CHEMBL5422245 — IC50 = 874.1 nM 6.06
CHEMBL5422930 — IC50 = 923.6 nM 6.04
CHEMBL5395241 — IC50 = 1060.0 nM 5.97
CHEMBL5410310 — IC50 = 1408.8 nM 5.85
CHEMBL5418320 — IC50 = 1541.2 nM 5.81
CHEMBL5417454 — IC50 = 1684.3 nM 5.77
CHEMBL5428017 — IC50 = 1705.0 nM 5.77