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Assay Detail

CHEMBL4427148

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Binding
Inhibition of KDM5 in human PC9 cells assessed as demethylation of H3K4Me3
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Liang J, Zhang B, Labadie S, Ortwine DF, Vinogradova M, Kiefer JR, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, Classon M, Trojer P, Dragovich PS, Murray L.
Bioorg Med Chem Lett (2016) 26 : 4036 -4041
PubMed 27406798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 5.45 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3785583 — — 1 6.47
CHEMBL4458334 — — 1 6.36
CHEMBL4542354 — — 1 6.06
CHEMBL4594120 — — 1 5.92
CHEMBL4469253 — — 1 5.89
CHEMBL4548921 — — 1 5.77
CHEMBL4464271 — — 1 5.75
CHEMBL4539736 — — 1 5.70
CHEMBL4587659 — — 1 5.64
CHEMBL4444473 — — 1 5.54
CHEMBL4518175 — — 1 5.17
CHEMBL4447703 — — 1 5.12
CHEMBL4450386 — — 1 5.08
CHEMBL4537301 — — 1 5.03
CHEMBL4516977 — — 1 4.95
CHEMBL4525674 — — 1 4.92
CHEMBL4468119 — — 1 4.86
CHEMBL4577929 — — 1 4.79
CHEMBL4470689 — — 1 4.55
CHEMBL4462289 — — 1 -
CHEMBL4551293 — — 1 -
CHEMBL4540055 — — 1 -
CHEMBL4589575 — — 1 -
CHEMBL4534100 — — 1 -
CHEMBL4435805 — — 1 -
CHEMBL4474549 — — 1 -
CHEMBL4483632 — — 1 -
CHEMBL4449759 — — 1 -
CHEMBL4457963 — — 1 -
CHEMBL4457381 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3785583 — EC50 = 340.0 nM 6.47
CHEMBL4458334 — EC50 = 440.0 nM 6.36
CHEMBL4542354 — EC50 = 870.0 nM 6.06
CHEMBL4594120 — EC50 = 1200.0 nM 5.92
CHEMBL4469253 — EC50 = 1300.0 nM 5.89
CHEMBL4548921 — EC50 = 1700.0 nM 5.77
CHEMBL4464271 — EC50 = 1800.0 nM 5.75
CHEMBL4539736 — EC50 = 2000.0 nM 5.70
CHEMBL4587659 — EC50 = 2300.0 nM 5.64
CHEMBL4444473 — EC50 = 2900.0 nM 5.54
CHEMBL4518175 — EC50 = 6700.0 nM 5.17
CHEMBL4447703 — EC50 = 7500.0 nM 5.12
CHEMBL4450386 — EC50 = 8300.0 nM 5.08
CHEMBL4537301 — EC50 = 9300.0 nM 5.03
CHEMBL4516977 — EC50 = 11300.0 nM 4.95
CHEMBL4525674 — EC50 = 12100.0 nM 4.92
CHEMBL4468119 — EC50 = 13800.0 nM 4.86
CHEMBL4577929 — EC50 = 16400.0 nM 4.79
CHEMBL4470689 — EC50 = 28400.0 nM 4.55
CHEMBL4468139 — EC50 > 30000.0 nM -
CHEMBL4548987 — EC50 - — -
CHEMBL4546025 — EC50 - — -
CHEMBL4518024 — EC50 - — -
CHEMBL4442998 — EC50 - — -
CHEMBL4564949 — EC50 - — -
CHEMBL4570968 — EC50 - — -
CHEMBL4434847 — EC50 > 30000.0 nM -
CHEMBL4544982 — EC50 > 30000.0 nM -
CHEMBL4534149 — EC50 - — -
CHEMBL4451492 — EC50 - — -
CHEMBL4444121 — EC50 > 30000.0 nM -
CHEMBL4567032 — EC50 > 30000.0 nM -
CHEMBL4457381 — EC50 - — -
CHEMBL4457963 — EC50 - — -
CHEMBL4449759 — EC50 - — -
CHEMBL4483632 — EC50 - — -
CHEMBL4474549 — EC50 - — -
CHEMBL4435805 — EC50 > 30000.0 nM -
CHEMBL4534100 — EC50 - — -
CHEMBL4589575 — EC50 - — -
CHEMBL4540055 — EC50 - — -
CHEMBL4551293 — EC50 - — -
CHEMBL4462289 — EC50 - — -