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Assay Detail

CHEMBL5217994

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

Binding
Inhibition of full-length P300 (unknown origin) using ARTKQTARKSTGGKAPRKQLAGG-K(Biotin)-amide as substrate preincubated for 60 mins followed by substrate addition and measured by RapdiFire-MS/MS analysis
28
Total Activities
28
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

Histone acetyltransferase p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Tian X, Suarez D, Thomson D, Li W, King EA, LaFrance L, Boehm J, Barton L, Di Marco C, Martyr C, Thalji R, Medina J, Knight S, Heerding D, Gao E, Nartey E, Cecconie T, Nixon C, Zhang G, Berrodin TJ, Phelps C, Patel A, Bai X, Lind K, Prabhu N, Messer J, Zhu Z, Shewchuk L, Reid R, Graves AP, McHugh C, Mangatt B.
J Med Chem (2022) 65 : 14391 -14408
PubMed 36302181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.56 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220994 1 10.10
CHEMBL5221053 1 10.00
CHEMBL5219157 1 9.90
CHEMBL5219030 1 9.80
CHEMBL5219693 1 9.80
CHEMBL5219667 1 9.70
CHEMBL5220447 1 9.60
CHEMBL5220732 1 9.60
CHEMBL5220956 1 9.50
CHEMBL5219678 1 9.40
CHEMBL5219512 1 9.20
CHEMBL5221030 1 9.10
CHEMBL5220546 1 9.10
CHEMBL5220332 1 9.00
CHEMBL5219466 1 8.70
CHEMBL5221088 1 8.30
CHEMBL5219851 1 8.10
CHEMBL5218875 1 8.00
CHEMBL5219712 1 8.00
CHEMBL5219204 1 7.80
CHEMBL5219472 1 7.70
CHEMBL5221117 1 7.70
CHEMBL5218882 1 7.40
CHEMBL5220135 1 7.30
CHEMBL5218485 1 7.10
CHEMBL5219575 1 7.00
CHEMBL1700017 1 6.80
CHEMBL5219253 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220994 IC50 = 0.07943 nM 10.10
CHEMBL5221053 IC50 = 0.1 nM 10.00
CHEMBL5219157 IC50 = 0.1259 nM 9.90
CHEMBL5219030 IC50 = 0.1585 nM 9.80
CHEMBL5219693 IC50 = 0.1585 nM 9.80
CHEMBL5219667 IC50 = 0.1995 nM 9.70
CHEMBL5220447 IC50 = 0.2512 nM 9.60
CHEMBL5220732 IC50 = 0.2512 nM 9.60
CHEMBL5220956 IC50 = 0.3162 nM 9.50
CHEMBL5219678 IC50 = 0.3981 nM 9.40
CHEMBL5219512 IC50 = 0.631 nM 9.20
CHEMBL5221030 IC50 = 0.7943 nM 9.10
CHEMBL5220546 IC50 = 0.7943 nM 9.10
CHEMBL5220332 IC50 = 1.0 nM 9.00
CHEMBL5219466 IC50 = 1.995 nM 8.70
CHEMBL5221088 IC50 = 5.012 nM 8.30
CHEMBL5219851 IC50 = 7.943 nM 8.10
CHEMBL5218875 IC50 = 10.0 nM 8.00
CHEMBL5219712 IC50 = 10.0 nM 8.00
CHEMBL5219204 IC50 = 15.85 nM 7.80
CHEMBL5219472 IC50 = 19.95 nM 7.70
CHEMBL5221117 IC50 = 19.95 nM 7.70
CHEMBL5218882 IC50 = 39.81 nM 7.40
CHEMBL5220135 IC50 = 50.12 nM 7.30
CHEMBL5218485 IC50 = 79.43 nM 7.10
CHEMBL5219575 IC50 = 100.0 nM 7.00
CHEMBL1700017 IC50 = 158.49 nM 6.80
CHEMBL5219253 IC50 = 1258.93 nM 5.90