Ki Summary

Reaction Details

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Target

Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1

Ligand

BDBM21025

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_143170 (CHEMBL744347)

IC50

9.0±n/a nM

Citation

Almquist, RG; Olsen, CM; Uyeno, ET; Toll, L Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity. J Med Chem27:115-20 (1984) [PubMed]

More Info.:

Get all data from this article, Assay Method

Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1

Name:

Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1

Synonyms:

Opioid receptor

Type:

n/a

Mol. Mass.:

n/a

Description:

ASSAY_ID of ChEMBL is 146137

Components:

This complex has 4 components.

Component 1

Name:

Sigma non-opioid intracellular receptor 1

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

25246.51

Organism:

Mus musculus (Mouse)

Description:

O55242

Residue:

223

Sequence:

MPWAAGRRWAWITLILTIIAVLIQAAWLWLGTQNFVFSREEIAQLARQYAGLDHELAFSR
LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCILHASLSEYVLLFGTALGSHGHSGRY
WAEISDTIISGTFHQWKEGTTKSEVFYPGETVVHGPGEATALEWGPNTWMVEYGRGVIPS
TLFFALADTFFSTQDYLTLFYTLRAYARGLRLELTTYLFGQDS

Component 2

Name:

Mu-type opioid receptor

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

44431.62

Organism:

MOUSE

Description:

OPIATE Mu OPRM1 MOUSE::P42866

Residue:

398

Sequence:

MDSSAGPGNISDCSDPLAPASCSPAPGSWLNLSHVDGNQSDPCGPNRTGLGGSHSLCPQT
GSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATST
LPFQSVNYLMGTWPFGNILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRT
PRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFA
FIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYV
IIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQ
QNSARIRQNTREHPSTANTVDRTNHQLENLEAETAPLP

Component 3

Name:

Kappa-type opioid receptor

Synonyms:

KOR-1 | MSL-1 | OPIATE Kappa | OPRK_MOUSE | Oprk1

Type:

Enzyme

Mol. Mass.:

42656.78

Organism:

Mus musculus (Mouse)

Description:

P33534

Residue:

380

Sequence:

MESPIQIFRGDPGPTCSPSACLLPNSSSWFPNWAESDSNGSVGSEDQQLESAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSAVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLASSVGISAIVLGGTKVREDVDVIECSLQFPDDEYSWWDLFMKICVFVFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITKLVLVVVAVFIICWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPVLYAFLDENFKRCFRDFCFPIKMRMERQSTNRV
RNTVQDPASMRDVGGMNKPV

Component 4

Name:

Delta-type opioid receptor

Synonyms:

DOR-1 | K56 | MSL-2 | OPIATE Delta | OPRD_MOUSE | Opioid receptors; mu and delta | Oprd1

Type:

Enzyme Catalytic Domain

Mol. Mass.:

40577.25

Organism:

MOUSE

Description:

P32300

Residue:

372

Sequence:

MELVPSARAELQSSPLVNLSDAFPSAFPSAGANASGSPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKLKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTQPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDINRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRTPCGRQEPGSLRRPRQATTRERVTAC
TPSDGPGGGAAA

BDBM21025

n/a

Name

BDBM21025

Synonyms:

(2R)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanamido]-4-methylpentanoic acid | (D-Ala2,D-Leu5)-Enkephalin | BW-180C | CHEMBL340032 | DADLE | DADLE-OH | H-Tyr-D-Ala-Gly-Phe-D-Leu-OH | [D-Ala2-D-Leu5]enkephalin

Type

ANALGESIC

Emp. Form.

C29H39N5O7

Mol. Mass.

569.6493

SMILES

CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(O)=O

Structure