Assay Detail

CHEMBL5701436

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

Binding

Binding affinity against GPATCH8 (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis

ChEMBL ↗

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Target

G patch domain-containing protein 8 (CHEMBL4523489) ↗

Open DB target context

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G patch domain-containing protein 8 (CHEMBL4523489) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target G patch domain-containing protein 8

CHEMBL4523489

Anchored from Assay target.

Protein identity G patch domain-containing protein 8

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

G patch domain-containing protein 8 (CHEMBL4523489) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, Huthmacher C, Gudgin E, Lugo D, Beinke S, Chapman TD, Roberts EJ, Soden PE, Auger KR, Mirguet O, Doehner K, Delwel R, Burnett AK, Jeffrey P, Drewes G, Lee K, Huntly BJ, Kouzarides T.
Nature (2011) 478 : 529 -533
PubMed 21964340 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	1	7.92	7.92

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0000565
EFO_TERM	EFO_TERM	-	—	leukemia

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1232461	MOLIBRESIB	2.0	1	7.92

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1232461	MOLIBRESIB	Kd	=	12.0	nM	7.92