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Assay Detail

CHEMBL4359588

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

Binding
Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay
ChEMBL ↗
51
Total Activities
51
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

Chromatin remodeling regulator CECR2 (CHEMBL3108639) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
Lucas SCC, Atkinson SJ, Bamborough P, Barnett H, Chung CW, Gordon L, Mitchell DJ, Phillipou A, Prinjha RK, Sheppard RJ, Tomkinson NCO, Watson RJ, Demont EH.
J Med Chem (2020) 63 : 5212 -5241
PubMed 32321240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.07 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465880 — — 1 8.20
CHEMBL4577486 — — 1 7.70
CHEMBL4514362 — — 1 7.50
CHEMBL4557734 — — 1 7.40
CHEMBL4518862 — — 1 7.30
CHEMBL4437578 — — 1 7.30
CHEMBL4436652 — — 1 7.20
CHEMBL4553980 — — 1 7.10
CHEMBL4467940 — — 1 7.10
CHEMBL4461164 — — 1 7.00
CHEMBL4589592 — — 1 6.90
CHEMBL4545743 — — 1 6.90
CHEMBL4576280 — — 1 6.90
CHEMBL4537897 — — 1 6.80
CHEMBL4446238 — — 1 6.70
CHEMBL4470476 — — 1 6.60
CHEMBL4542904 — — 1 6.60
CHEMBL4454840 — — 1 6.60
CHEMBL4463062 — — 1 6.60
CHEMBL4558839 — — 1 6.60
CHEMBL4449894 — — 1 6.50
CHEMBL4565203 — — 1 6.40
CHEMBL4521850 — — 1 6.30
CHEMBL4589461 — — 1 6.30
CHEMBL4590565 — — 1 6.00
CHEMBL4463848 — — 1 5.90
CHEMBL4584415 — — 1 5.80
CHEMBL4587991 — — 1 5.80
CHEMBL4588820 — — 1 5.80
CHEMBL4534331 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465880 — IC50 = 6.31 nM 8.20
CHEMBL4577486 — IC50 = 19.95 nM 7.70
CHEMBL4514362 — IC50 = 31.62 nM 7.50
CHEMBL4557734 — IC50 = 39.81 nM 7.40
CHEMBL4518862 — IC50 = 50.12 nM 7.30
CHEMBL4437578 — IC50 = 50.12 nM 7.30
CHEMBL4436652 — IC50 = 63.1 nM 7.20
CHEMBL4553980 — IC50 = 79.43 nM 7.10
CHEMBL4467940 — IC50 = 79.43 nM 7.10
CHEMBL4461164 — IC50 = 100.0 nM 7.00
CHEMBL4589592 — IC50 = 125.89 nM 6.90
CHEMBL4545743 — IC50 = 125.89 nM 6.90
CHEMBL4576280 — IC50 = 125.89 nM 6.90
CHEMBL4537897 — IC50 = 158.49 nM 6.80
CHEMBL4446238 — IC50 = 199.53 nM 6.70
CHEMBL4470476 — IC50 = 251.19 nM 6.60
CHEMBL4558839 — IC50 = 251.19 nM 6.60
CHEMBL4463062 — IC50 = 251.19 nM 6.60
CHEMBL4454840 — IC50 = 251.19 nM 6.60
CHEMBL4542904 — IC50 = 251.19 nM 6.60
CHEMBL4449894 — IC50 = 316.23 nM 6.50
CHEMBL4565203 — IC50 = 398.11 nM 6.40
CHEMBL4521850 — IC50 = 501.19 nM 6.30
CHEMBL4589461 — IC50 = 501.19 nM 6.30
CHEMBL4590565 — IC50 = 1000.0 nM 6.00
CHEMBL4463848 — IC50 = 1258.93 nM 5.90
CHEMBL4587991 — IC50 = 1584.89 nM 5.80
CHEMBL4588820 — IC50 = 1584.89 nM 5.80
CHEMBL4534331 — IC50 = 1584.89 nM 5.80
CHEMBL4584415 — IC50 = 1584.89 nM 5.80
CHEMBL4464650 — IC50 = 1995.26 nM 5.70
CHEMBL4457036 — IC50 = 3162.28 nM 5.50
CHEMBL4464057 — IC50 = 3981.07 nM 5.40
CHEMBL4441400 — IC50 = 3981.07 nM 5.40
CHEMBL4464309 — IC50 = 3981.07 nM 5.40
CHEMBL4445372 — IC50 = 3981.07 nM 5.40
CHEMBL4451776 — IC50 = 3981.07 nM 5.40
CHEMBL4555249 — IC50 = 5011.87 nM 5.30
CHEMBL4555757 — IC50 = 5011.87 nM 5.30
CHEMBL4454629 — IC50 = 6309.57 nM 5.20
CHEMBL4472174 — IC50 = 7943.28 nM 5.10
CHEMBL4525009 — IC50 = 7943.28 nM 5.10
CHEMBL4453574 — IC50 = 12589.25 nM 4.90
CHEMBL4562898 — IC50 = 19952.62 nM 4.70
CHEMBL4454864 — IC50 = 19952.62 nM 4.70
CHEMBL4568195 — IC50 = 25118.86 nM 4.60
CHEMBL4453989 — IC50 = 31622.78 nM 4.50
CHEMBL4567224 — IC50 = 79432.82 nM 4.10
CHEMBL4531037 — IC50 = 79432.82 nM 4.10
CHEMBL4442695 — IC50 > 100000.0 nM -