Assay Detail

CHEMBL5382353

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Binding

Displacement of FP-Probe from N-terminal His-tagged full length recombinant human HSET incubated for 2 hrs by fluorescence polarization based competitive binding assay

ChEMBL ↗

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Target

Kinesin-like protein KIFC1 (CHEMBL3351200) ↗

Open DB target context

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Kinesin-like protein KIFC1 (CHEMBL3351200) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Kinesin-like protein KIFC1

CHEMBL3351200

Anchored from Assay target.

Protein identity Kinesin-like protein KIFC1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Kinesin-like protein KIFC1 (CHEMBL3351200) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.

Saint-Dizier F, Matthews TP, Gregson AM, Prevet H, McHardy T, Colombano G, Saville H, Rowlands M, Ewens C, McAndrew PC, Tomlin K, Guillotin D, Mak GW, Drosopoulos K, Poursaitidis I, Burke R, van Montfort R, Linardopoulos S, Collins I.
J Med Chem (2023) 66 : 2622 -2645
PubMed 36749938 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	2	6.38	6.40
IC50	1	6.96	6.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5408867	—	—	1	6.96
CHEMBL14830	ADENOSINE DIPHOSPHATE	0.5	1	6.40
CHEMBL14249	ADENOSINE TRIPHOSPHATE	2.0	1	6.36

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5408867	—	IC50	=	109.0	nM	6.96
CHEMBL14830	ADENOSINE DIPHOSPHATE	Kd	=	400.0	nM	6.40
CHEMBL14249	ADENOSINE TRIPHOSPHATE	Kd	=	436.0	nM	6.36