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Assay Detail

CHEMBL5550985

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

Binding
Inhibition of 6His-tagged wild type CDK12/cyclin K (unknown origin) infected in insect cells incubated for 1 hr by TR-FRET assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

CDK12/Cyclin K (CHEMBL4106169)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements.
Hall A, Chatzopoulou M, Frost J.
Bioorg Med Chem (2024) 104 : 117653 -117653
PubMed 38579492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.29 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5573487 1 7.82
CHEMBL518800 1 7.80
CHEMBL461557 1 7.77
CHEMBL5575551 1 7.75
CHEMBL5575056 1 7.68
CHEMBL5594035 1 7.68
CHEMBL5565816 1 7.55
CHEMBL5568619 1 7.46
CHEMBL461556 1 7.44
CHEMBL5569096 1 7.44
CHEMBL5569293 1 7.39
CHEMBL5593913 1 7.36
CHEMBL5574391 1 7.34
CHEMBL5592449 1 7.24
CHEMBL5565299 1 7.22
CHEMBL5573271 1 7.11
CHEMBL5563303 1 6.74
CHEMBL5568703 1 6.61
CHEMBL5594597 1 6.22
CHEMBL14762 SELICICLIB 2.0 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5573487 EC50 = 15.0 nM 7.82
CHEMBL518800 EC50 = 16.0 nM 7.80
CHEMBL461557 EC50 = 17.0 nM 7.77
CHEMBL5575551 EC50 = 18.0 nM 7.75
CHEMBL5575056 EC50 = 21.0 nM 7.68
CHEMBL5594035 EC50 = 21.0 nM 7.68
CHEMBL5565816 EC50 = 28.0 nM 7.55
CHEMBL5568619 EC50 = 35.0 nM 7.46
CHEMBL461556 EC50 = 36.0 nM 7.44
CHEMBL5569096 EC50 = 36.0 nM 7.44
CHEMBL5569293 EC50 = 41.0 nM 7.39
CHEMBL5593913 EC50 = 44.0 nM 7.36
CHEMBL5574391 EC50 = 46.0 nM 7.34
CHEMBL5592449 EC50 = 57.0 nM 7.24
CHEMBL5565299 EC50 = 60.0 nM 7.22
CHEMBL5573271 EC50 = 78.0 nM 7.11
CHEMBL5563303 EC50 = 182.0 nM 6.74
CHEMBL5568703 EC50 = 246.0 nM 6.61
CHEMBL5594597 EC50 = 603.0 nM 6.22
CHEMBL14762 SELICICLIB EC50 = 703.0 nM 6.15