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Assay Detail

CHEMBL4427147

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Binding
Inhibition of KDM5A (unknown origin)
ChEMBL ↗
43
Total Activities
43
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

Lysine-specific demethylase 5A (CHEMBL2424504) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 43 7.70 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4594120 — — 1 8.28
CHEMBL4548921 — — 1 8.25
CHEMBL4518175 — — 1 8.21
CHEMBL4469253 — — 1 8.10
CHEMBL4435805 — — 1 8.04
CHEMBL4468119 — — 1 8.03
CHEMBL4525674 — — 1 8.02
CHEMBL4444473 — — 1 8.00
CHEMBL4468139 — — 1 8.00
CHEMBL4464271 — — 1 7.98
CHEMBL4587659 — — 1 7.96
CHEMBL4542354 — — 1 7.95
CHEMBL4567032 — — 1 7.92
CHEMBL4537301 — — 1 7.91
CHEMBL4516977 — — 1 7.89
CHEMBL4539736 — — 1 7.88
CHEMBL4444121 — — 1 7.88
CHEMBL4458334 — — 1 7.86
CHEMBL4447703 — — 1 7.86
CHEMBL3785583 — — 1 7.82
CHEMBL4577929 — — 1 7.81
CHEMBL4450386 — — 1 7.80
CHEMBL4457381 — — 1 7.76
CHEMBL4470689 — — 1 7.75
CHEMBL4434847 — — 1 7.75
CHEMBL4564949 — — 1 7.74
CHEMBL4551293 — — 1 7.70
CHEMBL4518024 — — 1 7.69
CHEMBL4546025 — — 1 7.69
CHEMBL4462289 — — 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4594120 — IC50 = 5.3 nM 8.28
CHEMBL4548921 — IC50 = 5.6 nM 8.25
CHEMBL4518175 — IC50 = 6.2 nM 8.21
CHEMBL4469253 — IC50 = 7.9 nM 8.10
CHEMBL4435805 — IC50 = 9.2 nM 8.04
CHEMBL4468119 — IC50 = 9.3 nM 8.03
CHEMBL4525674 — IC50 = 9.5 nM 8.02
CHEMBL4444473 — IC50 = 10.1 nM 8.00
CHEMBL4468139 — IC50 = 10.0 nM 8.00
CHEMBL4464271 — IC50 = 10.4 nM 7.98
CHEMBL4587659 — IC50 = 11.1 nM 7.96
CHEMBL4542354 — IC50 = 11.2 nM 7.95
CHEMBL4567032 — IC50 = 11.9 nM 7.92
CHEMBL4537301 — IC50 = 12.3 nM 7.91
CHEMBL4516977 — IC50 = 12.8 nM 7.89
CHEMBL4539736 — IC50 = 13.3 nM 7.88
CHEMBL4444121 — IC50 = 13.1 nM 7.88
CHEMBL4458334 — IC50 = 13.8 nM 7.86
CHEMBL4447703 — IC50 = 13.9 nM 7.86
CHEMBL3785583 — IC50 = 15.1 nM 7.82
CHEMBL4577929 — IC50 = 15.5 nM 7.81
CHEMBL4450386 — IC50 = 15.9 nM 7.80
CHEMBL4457381 — IC50 = 17.5 nM 7.76
CHEMBL4470689 — IC50 = 18.0 nM 7.75
CHEMBL4434847 — IC50 = 18.0 nM 7.75
CHEMBL4564949 — IC50 = 18.2 nM 7.74
CHEMBL4551293 — IC50 = 20.1 nM 7.70
CHEMBL4518024 — IC50 = 20.4 nM 7.69
CHEMBL4546025 — IC50 = 20.3 nM 7.69
CHEMBL4462289 — IC50 = 21.1 nM 7.68
CHEMBL4457963 — IC50 = 24.0 nM 7.62
CHEMBL4540055 — IC50 = 24.7 nM 7.61
CHEMBL4544982 — IC50 = 27.5 nM 7.56
CHEMBL4449759 — IC50 = 28.3 nM 7.55
CHEMBL4570968 — IC50 = 28.9 nM 7.54
CHEMBL4474549 — IC50 = 29.0 nM 7.54
CHEMBL4589575 — IC50 = 29.3 nM 7.53
CHEMBL4548987 — IC50 = 31.6 nM 7.50
CHEMBL4442998 — IC50 = 35.9 nM 7.45
CHEMBL4534149 — IC50 = 63.2 nM 7.20
CHEMBL4451492 — IC50 = 76.6 nM 7.12
CHEMBL4483632 — IC50 = 319.0 nM 6.50
CHEMBL4534100 — IC50 = 5400.0 nM 5.27